- Synthesis of Chromeno[2,3-d]pyrimidin-5-one Derivatives from 1,3,5-Triazinanes via Two Different Reaction Pathways
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1,3,5-Triazinanes, as a kind of versatile building block, are applied in the synthesis of chromeno[2,3-d]pyrimidin-5-one derivatives via two different reaction modes, which perfectly exhibits the powerful function of 1,3,5-triazinane as a three-atom synth
- Wang, Taimin,Zhang, Biwei,Hu, Lin,Sun, Haiyan,Wang, Yan,Zhai, Hongbin,Cheng, Bin
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p. 1348 - 1356
(2022/01/27)
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- Chromone dioxadiazole compound as well as preparation method and application thereof
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The preparation method comprises the following steps: adding an intermediate F and bis (acetoxy) iodobenzene to dichloromethane for reaction to obtain the chromone compound. The invention provides a novel chromone dioxadiazole compound and a preparation method thereof, and overcomes the defects of large toxicity and high preparation cost of the traditional method.
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Paragraph 0021-0023
(2021/10/30)
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- Synthesis and biological evaluation of chromone-3-carboxamides
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The aim of our study was to synthesize novel chromone-3-carboxamides and to conduct biological evaluations in search for lead compounds for the treatment of a range of debilitating disease states. Corresponding 2-hydroxyacetophenones were subjected to Vilsmeier-Haack formylation to give chromone-3-carbaldehydes, which were subsequently oxidised to give chromone-3-carboxylic acids. Treatment of the carboxylic acids with thionyl chloride resulted in the in situ formation of the corresponding acid chlorides, which were reacted with various amines in the presence of triethylamine to give the corresponding novel chromone-3-carboxamides in good yields. Selected chromone derivatives were then evaluated for their anti-inflammatory, anti-tryponosomal and cytotoxic properties.
- Gordon, Allen T.,Ramaite, Isaiah D.I.,Mnyakeni-Moleele, Simon S.
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p. 148 - 160
(2021/01/20)
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- Novel p-functionalized chromen-4-on-3-yl chalcones bearing astonishing boronic acid moiety as MDM2 inhibitor: Synthesis, cytotoxic evaluation and simulation studies
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Background: Novel 4-[3-(6/7/8-Substituted 4-Oxo-4H-chromen-3-yl)acryloyl]phenyl-boronic acid derivatives (5a-h) as well as other 6/7/8-substituted-3-(3-oxo-3-(4-substituted-phenyl)prop-1-enyl)-4H-chromen-4-one derivatives (3a-u) have been designed as p53-MDM2 pathway inhibitors and reported to possess significant cytotoxic properties against several cancer cell lines. Objectives: The current project aims to frame the structure-anticancer activity relationship of chromen-4-on-3-yl chalcones (3a-u/5a-h). In addition, docking studies were performed on these chromeno-chalcones in order to have an insight into their interaction possibilities with MDM2 pro-tein. Methods: Twenty-nine chromen-4-on-3-yl chalcone derivatives (3a-u/5a-h) were prepared by utilizing silica supported-HClO4 (green route with magnificent yield) and tested against four cancer cell lines (HCT116, MCF-7, THP-1, NCIH322). Results: Among the series 3a-u, compound 3b exhibited the highest anticancer activity (with IC50 values ranging from 8.6 to 28.4 μM) overall against tested cancer cell lines. Interestingly, para-Boronic acid derivative (5b) showed selective inhibition against colon cancer cell line, HCT-116 with an IC50 value of 2.35 μM. Besides the emblematic hydrophobic interactions of MDM2 inhibi-tors, derivative 5b was found to exhibit extra hydrogen bonding with GLN59 and GLN72 residues of MDM2 in molecular dynamics (MD) simulation. All the compounds were virtually nontoxic against normal fibroblast cells. Conclusion: Novel compounds were obtained with good anticancer activity especially 6-Chlorochromen-4-one substituted boronic acid derivative 5b. The molecular docking study proposed good activity as a MDM-2 inhibitor suggesting hydrophobic as well as hydrogen bonding interactions with MDM2.
- Bhatia, Richa Kaur,Coutinho, Evans C.,Garg, Ruchika,Kancherla, Satyavathi,Kaur, Maninder,Madan, Jitender,Pissurlenkar, Raghuvir R. S.,Singh, Lakhwinder,Yadav, Manmohan
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p. 212 - 228
(2020/03/10)
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- NHC-Catalyzed Cascade Reaction between β-Methyl Enals and Dienones for Quick Construction of Complex Multicyclic Lactones
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A NHC-promoted cascade reaction between β-methyl enal and dienone is developed for quick access to multicyclic lactone molecules bearing quaternary chiral carbon centers. Our study constitutes the first 1,6-addition of the acylazolium vinyl enolate γ-carbon via NHC catalysis and provides rapid access to complex lactone molecules that are otherwise difficult to prepare. The structurally sophisticated lactone products bearing up to four fused ring structures are afforded in up to quantitative yields with good to excellent enantioselectivities.
- Sun, Jun,Xu, Jun,Nie, Guihua,Jin, Zhichao,Chi, Yonggui Robin
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supporting information
p. 2595 - 2599
(2020/03/30)
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- Synthesis, characterization and biological activity of mixed ligands complexes of quinolin-8-ol and substituted chromones with Mn(II), Co(II), Ni(II) and Cu(II) metal ions
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The mixed ligand complexes were synthesized using quinolin-8-ol and substituted chromone derivative with transition metals like Mn(II), Cu(II), Ni(II) and Co(II). These complexes were characterized using elemental analysis by electron dispersive spectroscopy, Fourier transforms infrared, ultraviolet–visible, proton nuclear magnetic resonance, liquid chromatography coupled with mass spectrometry, electron spin resonance spectra, magnetic susceptibility, powder X-ray diffraction, thermogravimetric analysis and scanning electron microscopy. The complexes were screened by biological activities such as antioxidant activity by 2, 2-Diphenyl-1-picrylhydrazyl, antimicrobial activity by the agar well-diffusion method and anticancer activity by yellow tetrazolium (3-(4, 5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide methods. The synthesis of mixed ligand complexes were synthesized by using homoleptic complexes of respective metal complexes of chromones. The FTIR spectra show νM–O the νM–N frequencies are obtained at 515–645?cm?1 and 431–496?cm? 1 respectively. The NMR spectra of Ni(II) complexes were indicating the complexes are paramagnetic in nature. The ESR spectra of copper complexes shows singlet signal, and they indicate that the copper has 2 + oxidation state in complexes. The complexes showed a well-defined crystal system indicated by powder-X-ray diffraction patterns. The thermogram studies show formation of metal oxides residues at the end product of decomposition of complexes. The scanning electron microscope showed complexes were nanocrystalline in nature. The mixed ligand complex of Ni(II) shows 80.73% antioxidant activity as compared to both the ligands and other metal complexes. The antibacterial activity result obtained clearly showed that all complexes were effective against all the microorganisms of Staphylococcus aures, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginos. The inhibition of the cancerous cell is more the case of Ni (II) complexes as compared with other complexes.
- Kolhe, Nitin H.,Jadhav, Shridhar S.
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p. 973 - 996
(2018/11/23)
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- One pot and metal-free approach to 3-(2-Hydroxybenzoyl)-1-aza-anthraquinones
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Herein, a direct strategy to synthesize 3-(2-hydroxybenzoyl)-1-aza-anthraquinones with excellent efficiency,mild conditions, and benign functional group compatibilitywas reported. Avariety of 3-formylchromone compounds were employed as compatible substrates and this protocol gave the 3-(2-hydroxybenzoyl)-1-aza-anthraquinone derivatives in good to excellent yields without inert gas and expensive transition metal catalysts. Some compounds displayed good anti-proliferative activities.
- Yuan, Jiaqi,He, Qian,Song, Shanshan,Zhang, Xiaofei,Miao, Zehong,Yang, Chunhao
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supporting information
(2019/08/30)
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- Synthesis and Antimicrobial Activity of (Z)-3-{[3-Oxobenzofuran-2(3H)-ylidene]methyl}-4H-chromen-4-one Derivatives
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A series of (Z)-3-{[3-oxobenzofuran-2(3H)-ylidene]methyl}-4H-chromen-4-one derivatives have been synthesized from 2-hydroxyl acetophenones by the Vilesmeier–Haack reaction, Claisen–Schmidt reaction and mercury(II) acetate/cupric bromide. All the synthesized compounds were characterized by IR, 1H and 13C NMR, and mass spectral data and elemental analysis. The products were tested for their in vitro antimicrobial activity.
- Pervaram,Ashok,Reddy,Sarasija,Rao
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p. 566 - 572
(2018/04/23)
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- Hydrazide derivatives and anticancer agent comprising the same
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The present invention relates to novel hydrazide derivatives, pharmaceutically-acceptable salt of the same, a pharmaceutical composition including the hydrazide derivatives for prevention and treatment of cancer, and a dietary supplement composition inclu
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Paragraph 0148-0150
(2019/02/20)
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- Direct construction of xanthene and benzophenone derivatives via Br?nsted acid controlled Diels-Alder reaction of 3-vinylchromones and arynes
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A Br?nsted acid controlled Diels-Alder reaction of 3-vinylchromones with arynes has been developed. By employing different kinds and amounts of acid, 9-aryl-9H-xanthen-9-ols or ortho-hydroxybenzophenones could be controllably furnished in good yields in an atom- and step-economic manner.
- Huang, Xu-Jiao,Tao, Yuan,Li, Yue-Kun,Wu, Xin-Yan,Sha, Feng
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supporting information
p. 8565 - 8577
(2016/12/09)
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- Synthesis and biological evaluation of N-Aryl-N′-(5-(2-hydroxybenzoyl) pyrimidin-2-yl)guanidines as toll-like receptor 4 antagonists
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Background: Toll-like receptor 4 (TLR4) has been associated with several inflammatory diseases, such as sepsis, atherosclerosis and chronic pain. Objective: The aim of the present study was to develop an efficient and straightforward synthetic approach for the preparation of small-molecule antagonists Naryl-N′-(5-(2-hydroxybenzoyl)pyrimidin-2-yl)guanidines in order to evaluate these for TLR4 antagonist activity and to obtain useful information about their structure-activity relationships. Methods: The present work have designed and optimized a three-step synthetic route for derivatives of a previously demonstrated antagonist of TLR4: 1-(4-fluorophenyl)-2-(5-(2-hydroxy-5-methoxybenzoyl)pyrimidin-2-yl)guanidine. The antagonist activities of eight novel synthesized compounds were evaluated on cells which selectively express TLR4. Results: Three guanidine derivatives showed promising antagonist activities, with IC50 values in the low micromolar range. Conclusion: Our findings represent an important starting point for further studies of small-molecule agents targeting Toll-like receptors.
- Sova, Matej,Ro?man, Kaja,?vajger, Urban,Ro?man, Primo?,Gobec, Stanislav
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p. 742 - 750
(2016/11/29)
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- Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors
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Two series of thienopyrimidine derivatives (10a-k, 16a-j) bearing chromone moiety were designed and synthesized. All the compounds were evaluated for inhibitory activity against mTOR kinase at a concentration of 10uM. Four selected compounds were further evaluated for the IC50 values against mTOR kinase, PI3Kα kinase and two cancer cell lines. Some of the target compounds exhibited moderate to excellent mTOR/PI3Kα kinase inhibitory activity and cytotoxicity. The most promising compound 16i showed good inhibitory activity against mTOR/PI3Kα kinase and good antitumor potency for H460 and PC-3 cell lines with IC50 values of 0.16 ± 0.03 μM, 2.35 ± 0.19 μM, 1.20 ± 0.23 μM and 0.85 ± 0.04 μM, which were 8.6, >5, 7.9 and 19.1 times more active than compound I (1.37 ± 0.07 μM, >10 μM, 9.52 ± 0.29 μM, 16.27 ± 0.54 μM), respectively. Structure-activity relationships (SARs) and docking studies indicated that the chromone moiety is necessary for the potent antitumor activity and cytotoxicity of these compounds. Substitution of the chromone moiety at the 6-position has a significant impact to the inhibitory activity, in particular a carboxylic acid group, produced the best potency.
- Zhu, Wufu,Chen, Chen,Sun, Chengyu,Xu, Shan,Wu, Chunjiang,Lei, Fei,Xia, Hui,Tu, Qidong,Zheng, Pengwu
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- Thiazolidine-2,4-diones derivatives as PPAR-γ agonists: Synthesis, molecular docking, in vitro and in vivo antidiabetic activity with hepatotoxicity risk evaluation and effect on PPAR-γ gene expression
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A library of conjugates of chromones and 2,4-thiazolidinedione has been synthesized by Knoevenagel condensation followed by reduction using hydrogen gas and Pd/C as a catalyst. Compounds 5c and 5e were most effective in lowering the blood glucose level comparable to standard drug pioglitazone. Compound 5e exhibited potent PPAR-γ transactivation of 48.72% in comparison to pioglitazone (62.48%). All the molecules showed good glide score against the PPAR-γ target in molecular docking study. PPAR-γ gene expression was significantly increased by compound 5e (2.56-fold) in comparison to standard drug pioglitazone. Compounds 5e and 5c did not cause any damage to the liver and may be considered as promising candidates for the development of new antidiabetic agents.
- Nazreen, Syed,Alam, Mohammad Sarwar,Hamid, Hinna,Yar, Mohammad Shahar,Dhulap, Abhijeet,Alam, Perwez,Pasha,Bano, Sameena,Alam, Mohammad Mahboob,Haider, Saqlain,Kharbanda, Chetna,Ali, Yakub,Pillai
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p. 3034 - 3042
(2014/06/24)
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- Combining QSAR classification models for predictive modeling of human monoamine oxidase inhibitors
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Due to their role in the metabolism of monoamine neurotransmitters, MAO-A and MAO-B present a significant pharmacological interest. For instance the inhibitors of human MAO-B are considered useful tools for the treatment of Parkinson Disease. Therefore, the rational design and synthesis of new MAOs inhibitors is considered of great importance for the development of new and more effective treatments of Parkinson Disease. In this work, Quantitative Structure Activity Relationships (QSAR) has been developed to predict the human MAO inhibitory activity and selectivity. The first step was the selection of a suitable dataset of heterocyclic compounds that include chromones, coumarins, chalcones, thiazolylhydrazones, etc. These compounds were previously synthesized in one of our laboratories, or elsewhere, and their activities measured by the same assays and for the same laboratory staff. Applying linear discriminant analysis to data derived from a variety of molecular representations and feature selection algorithms, reliable QSAR models were built which could be used to predict for test compounds the inhibitory activity and selectivity toward human MAO. This work also showed how several QSAR models can be combined to make better predictions. The final models exhibit significant statistics, interpretability, as well as displaying predictive power on an external validation set made up of chromone derivatives with unknown activity (that are being reported here for first time) synthesized by our group, and coumarins recently reported in the literature.
- Helguera, Aliuska Morales,Perez-Garrido, Alfonso,Gaspar, Alexandra,Reis, Joana,Cagide, Fernando,Vina, Dolores,Cordeiro, M.Natalia D.S.,Borges, Fernanda
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- Novel benzofuran-chromone and -coumarin derivatives: Synthesis and biological activity in K562 human leukemia cells
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Not widely distributed in nature, aurones, (Z)-2-benzylidene-benzofuran- 3(2H)-ones, are one of the less common and lesser-known representatives of a flavonoid subclass. Nevertheless, they exhibit a strong and broad variety of biological activities. We have combined the benzofuranone part of a classical aurone with either a chromone or a coumarin scaffold which proved to feature interesting biological activities including antimicrobial, antiviral, anticancer, anti-inflammatory and antioxidant properties. Herein we present a series of 26 novel benzofuran derivatives with the first biological results in K562 human leukemia cells showing that compounds 21b, 29b and 29c are able to induce around 24% apoptosis.
- Zwergel, Clemens,Valente, Sergio,Salvato, Angela,Xu, Zhanjie,Talhi, Oualid,Mai, Antonello,Silva, Artur,Altucci, Lucia,Kirsch, Gilbert
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supporting information
p. 1571 - 1579
(2013/12/04)
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- Design and syntheses of novel N′-((4-oxo-4H-chromen-3-yl)methylene) benzohydrazide as inhibitors of cyanobacterial fructose-1,6-/sedoheptulose-1,7- bisphosphatase
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Cyanobacterial fructose-1,6-/sedoheptulose-1,7-bisphoshatase (Cy-FBP/SBPase) is an important target enzyme for finding inhibitors to solve harmful algal bloom (HAB). In this study, as potential inhibitors of Cy-FBP/SBPase, a series of novel chromone-connecting benzohydrazone compounds (Novel N′-((4-oxo-4H-chromen-3-yl)methylene)benzohydrazide) were designed and synthesized. Their inhibitory activities against Cy-FBP/SBPase were further examined in vitro. Some of these compounds, such as f6-f8, f11, f12 and f16, exhibit higher inhibitory activities (IC50 = 11.2-16.1 μM), especially, the compound f7 was identified as the most potent inhibitor with IC50 value of 11.2 μM. The probable binding-mode of compound f7 was further analyzed carefully by molecular docking methods. These results indicate that compound f7 could be used as a lead compound for further optimization and might have potential to be developed as a new algicide.
- Tu, Qi-Dong,Li, Ding,Sun, Yao,Han, Xin-Ya,Yi, Fan,Sha, Yibamu,Ren, Yan-Liang,Ding, Ming-Wu,Feng, Ling-Ling,Wan, Jian
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p. 2826 - 2831
(2013/06/27)
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- 3-Formylchromone based topoisomerase IIα inhibitors: Discovery of potent leads
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Substituted 3-formylchromones were synthesized and evaluated as inhibitors of the human DNA topoisomerase IIα (hTopo-IIα) enzyme. The results of the decatenation, relaxation and DNA intercalation assays revealed that the compounds (11b, 12a, 12b, 12d, 12e, 13a and 13b) exhibited potent inhibitory activity against the hTopo-IIα enzyme, and are nonintercalating agents. These compounds also possess significant in vitro cytotoxicity (LC50 ranges from 0.5-8.6 μM) against prostate (PC-3) cancerous cell line as seen in comparison to the standard drug etoposide. To further probe the plausible mode of action of 3-formylchromone derivatives, molecular docking studies have also been carried out, which showed that the compounds under investigation fitted well in the ATP binding pocket of hTopo-IIα enzyme with good docking scores and form nonbonding interactions with the crucial residues of the catalytic site. The Royal Society of Chemistry.
- Singh, Satyajit,Baviskar, Ashish Triambak,Jain, Vaibhav,Mishra, Nidhi,Chand Banerjee, Uttam,Bharatam, Prasad V.,Tikoo, Kulbhushan,Singh Ishar, Mohan Paul
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supporting information
p. 1257 - 1266
(2013/09/12)
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- One-pot syntheses of novel pyrazole-containing bisphosphonate esters at room temperature
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An efficient general synthetic approach has been developed to synthesize pyrazole-containing bisphosphonate (N-BPs) esters from chromenone derivatives via a sequential two-step reaction in one pot at ambient temperature in good to excellent yields. This protocol provides a new convenient method to prepare lipophilic bisphosphonate precursors with potential activities. The Royal Society of Chemistry 2012.
- Xiang, Haoyue,Qi, Xueyu,Xie, Yuyuan,Xu, Guangyu,Yang, Chunhao
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supporting information
p. 7730 - 7738
(2013/04/23)
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- Synthesis and characterization and anti-inflammatory and antibacterial evaluation of 3-arylidene-7-methoxychroman-4-ones
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3-Arylidene-7-methoxychroman-4-ones 3a-k have been prepared from 7-methoxy-chroman-4-one 1 and heterocyclic aldehydes 2 and have been evaluated for anti-inflammatory and antibacterial activities. All of them have registered moderate anti-inflammatory and antibacterial activities.
- Shankar,Gandhidasan,Venkataraman
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experimental part
p. 1202 - 1207
(2011/10/13)
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- Synthesis of 3-[3-(benzothiazol-2-yl)-4-oxo-thiazolidin-2-yl]chromones as Antifungal agents
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Antifungal activities associated with chromones and thiazolidones prompted us to synthesize 3-[3-(benzothiazol-2-yl)-4-oxo-thiazolidin-2-yl]chromones through the intermediacy of Schiff bases. Structures of new compounds have been assigned by the interpretation of their IR and PMR spectral data and are supported by elemental analysis. One of the Schiff base adduct has shown high antifungal activity (90.93 % inhibition of growth) against Aspergillus niger i.e., the fungus responsible for food poisoning and aspergillosis. It is worth mentioning as the isolation and purification of Schiff bases was not easy due to 1,4-adduct formation. Hence, a one pot synthesis of title compounds was designed by refluxing a mixture of 3-formylchromone, 2-aminobenzothiazole and thioglycollic acid (TGA) in benzene in presence of zinc chloride instead of reacting Schiff base with thioglycollic acid.
- Sharma, Vinay Prabha,Kumar, Praveen,Sharma, Meenakshi
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body text
p. 4616 - 4620
(2012/02/04)
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- Catalytic effects in baylis-hillman reactions of chromone-3-carbaldehydes with acrylonitrile and methyl acrylate
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The effects of various catalysts, the solvent system, and the temperature on the efficiency and chemoselectivity of reactions of a series of chromone-3-carbaldehydes with acrylonitrile and methyl acrylate are discussed.
- Molefe, Duduzile M.,Kaye, Perry T.
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scheme or table
p. 3586 - 3600
(2009/12/09)
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- Chromone studies. Part 17. Tricyclic scaffolds from reactions of chromone- 3-carbaldehydes and methyl vinyl ketone under Baylis-Hillman conditions
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Reaction of a series of chromone-3-carbaldehydes with methyl vinyl ketone under Baylis-Hillman conditions, sing 3-hydroxyquinuclidine in chloroform or DABCO in 1-methyl-2-pyrrolidinone, affords unprecedented tricylic hromone derivatives which, depending on the conditions, may be accompanied by the normal Baylis-Hillman roducts or their respective tricycl ic dimers.
- Molefe, Duduzile M.,Ganto, Mlungiseleli M.,Lobb, Kevin A.,Kaye, Perry T.
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scheme or table
p. 452 - 456
(2010/01/16)
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- Microwave-induced synthesis and regio- and stereoselective epoxidation of 3-styrylchromones
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The microwave-assisted solvent-free synthesis of (E)-3-styrylchromones from 3-formylchromones and phenylmalonic acid on sodium acetate support has been developed; the method affords the styryl derivatives in moderate to good yields and with complete diastereoselectivity. Protocols for the highly regioselective epoxidation of (E)- and (Z)-3-styrylchromones have been elaborated. Treatment of the alkenes with dimethyldioxirane led to the exclusive formation of 3-(3-aryloxiran-2-yl)chromones with complete diastereoselectivity, whereas treatment with hydrogen peroxide under alkaline conditions afforded the corresponding 2,3-epoxy-3-styrylchromanones as the only products. Epoxidation performed in the presence of chiral, nonracemic cinchona-alkaloid-based quaternary ammonium salts allowed the synthesis of enantiomerically enriched 2,3-epoxy-3-styrylchromanones, but with only moderate ee values. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Patonay, Tamas,Kiss-Szikszai, Attila,Silva, Vera M. L.,Silva, Artur M. S.,Pinto, Diana C. G. A.,Cavaleiro, Jose A. S.,Jeko, Jozsef
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body text
p. 1937 - 1946
(2009/04/04)
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- Synthesis and reactivity of 3-(1-hydroxy-3-buten-1-yl)chromone
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Zn-induced allylation of chromone-3-carbaldehyde 1 produces 3-(1-hydroxy-3-butene-1-yl)chromone 2, which gives back 1 on treatment with formalin under acidic conditions, and reacts differently towards nitrogenous nucleophiles.
- Karmakar, Partha,Ghosh, Tarun,Chakrabarty, Debasish,Maiti, Sourav,Bandyopadhyay, Chandrakanta
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experimental part
p. 208 - 211
(2009/08/07)
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- Synthesis and insecticidal activity of chromanone and chromone analogues of diacylhydrazines
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Diacylhydrazine derivatives have been identified as one of the most important insect growth regulators. A variety of diacylhydrazine derivatives were designed and synthesized in recent years due to their unique action mechanism, simple structure, and environmental benign character. This paper describes the molecular design, synthesis, and insecticidal activities of a series of chromanone and chromone analogues of diacylhydrazine derivatives. The preliminary bioassay showed that some of the chromanone analogues exhibited good insecticidal activity against Mythima separata at the dosage of 500 mg L-1. The present work demonstrated that replacement of the chroman ring of ANS-118, a commercial insecticide, with chromanone moiety could result in new compounds with high potent insecticidal activity.
- Zhao, Pei-Liang,Li, Jing,Yang, Guang-Fu
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p. 1888 - 1895
(2007/10/03)
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- Design, synthesis, and evaluation of novel 6-chloro-/fluorochromone derivatives as potential topoisomerase inhibitor anticancer agents
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6-Chloro-2-pyrrolidino-/morpholino-/piperidino-/N-methylpiperazino-3- formyl-chromones (13-16) and 6-fluoro-2,7-di-morpholino-/piperidino-/N- methylpiperazino-3-formylchromones (17-19) have been synthesized as potential topoisomerase inhibitor anticancer agents, and evaluated, in vitro, against Ehrlich ascites carcinoma (EAC) cells, and also in vivo on EAC bearing mice. The compounds displayed promising anticancer activity under these test systems and shall serve as useful 'leads' for further design.
- Ishar,Singh, Gurpinder,Singh, Satyajit,Sreenivasan,Singh, Gurmit
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p. 1366 - 1370
(2007/10/03)
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- Ceric ammonium nitrate catalyzed efficient and chemoselective method for protection and deprotection of 4-oxo-4H-1-benzopyran-3-carbaldehydes
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A chemoselective, solvent-free, mild and efficient method for the synthesis of acylals and their deprotection to 4-oxo-4H-1-benzopyran-3-carbaldehydes catalyzed by ceric ammonium nitrate (CAN) are carried out in good yields and all compounds 2a-h are characterized by IR, 1H NMR and 13C NMR spectral data.
- Shindalkar,Madje,Hangarge,Shingare
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p. 2409 - 2411
(2007/10/03)
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- Diels-Alder reactions of chromone-3-carboxaldehydes with ortho-benzoquinodimethane. New synthesis of benzo[b]xanthones
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An efficient new route to the benzo[b]xanthone system has been developed and applied to the synthesis of several new derivatives. The cycloaddition reactions of chromone-3-carboxaldehydes 12, reacting as dienophiles, with ortho-benzoquinodimethane 7 gave a diastereomeric mixture of cycloadducts 8 and 9. The formation of these compounds results from the Diels-Alder reactions of 12 and 7 followed by the in situ deformylation. The oxidation of adducts 8 and 9 with dimethyl sulfoxide in the presence of iodine gave the novel benzo[b]xanthones 11 in good yields.
- Sandulache, Angela,Silva, Artur M.S,Cavaleiro, José A.S
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p. 105 - 114
(2007/10/03)
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- 2-Hydroxy Ketones, V. --- Preperation of Substituted Chromones
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Various 2-hydroxyacetophenone derivatives react with Vilsmeier reagent according to the Harnisch method to give the substituted chromones 2b-i, which have been identified by elemental analyses and IR and 1H-NMR spectra.
- Cascaval, Alexandru
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p. 669 - 672
(2007/10/02)
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- Chromonealdehyde compounds and process for the production thereof
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There are provided compounds of the general formula SPC1 Wherein R is a hydroxy, alkyl, acyloxy, halogen, nitro, substituted or unsubstituted amino, alkoxy, carboxy or a group derived from a carboxy group and m is 0, 1 or 2 except where m is 2, the two R groups are both hydroxy groups. The present invention is also concerned with a process for preparing the chromonealdehyde compounds. The chromonealdehyde compounds are characterized by antiallergic properties and are therefore useful as prophylactic and therapeutic agents for allergic asthma, allergic dermatitis and other allergic diseases and also are valuable as intermediates for the synthesis of other pharmaceutical compounds having the chromone nucleus.
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