- Method for efficiently synthesizing 1, 3-bis (4-hydroxyphenyl)-2-propylene-1-ketone
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The invention discloses a method for efficiently synthesizing 1, 3-bis (4-hydroxyphenyl)-2-propene-1-ketone, and belongs to the field of organic chemical synthesis. According to the method, a Claisen-Schmidt reaction is carried out, p-hydroxybenzaldehyde
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Paragraph 0024-0031
(2021/01/29)
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- Antibacterial and anti-inflammatory activity of valproic acid-pyrazole conjugates as a potential agent against periodontitis
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Periodontitis is a serious global concern. Therefore, in the present study, we intend to synthesize novel valproic-acid pyrazole conjugates as a novel agent against periodontitis. The molecules were developed in a facile synthetic route and obtained in ex
- Dai, Xinxiang,Dong, Lei,Fang, Ling,Wang, Jia,Xu, Pei,Zhang, Jia
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- Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia
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Based on hit-likeness and chemical diversity, a number of chalcones and chalcone-mimetic compounds were selected as putative Notch inhibitors. The evaluation of the antiproliferative effect combined with the inhibition of Notch1 expression in KOPTK1 cell line identified compound 18, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.
- Quaglio, Deborah,Zhdanovskaya, Nadezda,Tobajas, Gloria,Cuartas, Viviana,Balducci, Silvia,Christodoulou, Michael S.,Fabrizi, Giancarlo,Gargantilla, Marta,Priego, Eva-María,Carmona Pestania, álvaro,Passarella, Daniele,Screpanti, Isabella,Botta, Bruno,Palermo, Rocco,Mori, Mattia,Ghirga, Francesca,Pérez-Pérez, María-Jesús
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supporting information
p. 639 - 643
(2019/04/25)
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- Crosslinking Monomers With at Least One Sulfur Atom
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The invention relates to a cross-linking monomer with at least one sulfur atom, representable by a structure of formula (I) wherein the symbols have the following meaning: L1 is a linear, branched or cyclic, saturated or unsaturated, aliphatic
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Paragraph 0208; 0209
(2019/01/24)
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- BENZOXAZINES WITH PHOTO-CURABLE LINKAGES, THERMOSETS THEREOF, AND PREPARATION OF THE SAME
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The subject invention provides benzoxazines with photo-curable linkages, thermosets thereof, and preparation methods of the same. The compounds of the subject invention can be used in manufacture of many kinds of cross-linking polymer material, and the obtained material is improved in terms of many properties, especially high thermal properties. Moreover, the preparation method of the subject invention can precisely synthesize the targeted products by simply steps.
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Page/Page column 12
(2021/01/12)
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- Triaryl Pyrazole Toll-Like Receptor Signaling Inhibitors: Structure–Activity Relationships Governing Pan- and Selective Signaling Inhibitors
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The immune system uses members of the toll-like receptor (TLR) family to recognize a variety of pathogen- and host-derived molecules in order to initiate immune responses. Although TLR-mediated, pro-inflammatory immune responses are essential for host defense, prolonged and exaggerated activation can result in inflammation pathology that manifests in a variety of diseases. Therefore, small-molecule inhibitors of the TLR signaling pathway might have promise as anti-inflammatory drugs. We previously identified a class of triaryl pyrazole compounds that inhibit TLR signaling by modulation of the protein–protein interactions essential to the pathway. We have now systematically examined the structural features essential for inhibition of this pathway, revealing characteristics of compounds that inhibited all TLRs tested (pan-TLR signaling inhibitors) as well as compounds that selectively inhibited certain TLRs. These findings reveal interesting classes of compounds that could be optimized for particular inflammatory diseases governed by different TLRs.
- Pollock, Julie A.,Sharma, Naina,Ippagunta, Sirish K.,Redecke, Vanessa,H?cker, Hans,Katzenellenbogen, John A.
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p. 2208 - 2216
(2018/09/25)
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- Photo-sensitive benzoxazine II: Chalcone-containing benzoxazine and its photo and thermal-cured thermoset
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A chalcone-containing benzoxazine (BHP-a) was synthesized from a chalcone-containing bisphenol: 1,3-bis(4-hydroxyphenyl) propanone (BHP), aniline and paraformaldehyde in a co-solvent of xylene/1-butanol (2/1, V/V). The structure of BHP-a was successfully
- Lin, Ching Hsuan,Chien, Chun Kai,Chen, Chien Han,Juang, Tzong Yuan
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p. 37844 - 37851
(2017/08/18)
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- Synthesis and biological activity of 2,4-di-p-phenolyl-6-2-furanyl-pyridine as a potent topoisomerase II poison
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Dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives were simply achieved using Claisen-Schmidt condensation reaction and modified Kr?hnke pyridine synthetic method. Total forty-five compounds were designed and synthesized which contain hydroxyl groups
- Karki, Radha,Park, Chanmi,Jun, Kyu-Yeon,Kadayat, Tara Man,Lee, Eung-Seok,Kwon, Youngjoo
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p. 360 - 378
(2015/03/18)
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- The mesomorphic properties of chalcone dimer derivatives
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A homologous series of symmetrical dimers viz bis (4-n-alkoxy benzoyloxy) -phenyl β-benzoyl-ethylenes was synthesized and studied with a view to understanding the relation between molecular structure and the mesomorphic behavior. Twelve members of the dimeric series were synthesized, and the methoxy to butyloxy homologues are not liquid crystals, but the pentyloxy to hexadecyloxy are liquid crystals. The pentyl to heptyl dimers are only nematogenic, but the higher homologues show smectogenic mesomorphism prior to nematogenic mesophase formation. The phase diagram of phase transition curves behaves in a normal manner except for the smectic to nematic transition curve which behaves in an unexpected manner. The smectic and nematic thermal stabilities are 103°C and 131.7°C, respectively. The smectogenic and nematogenic phase lengths vary between 17.4°C to 28.3°C and 2.1°C to 29.9°C, respectively. The liquid crystal properties of presently investigated novel chalcone dimers are compared with known monomeric chalcones.
- Kotadiya,Bhoya
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p. 116 - 124
(2015/03/18)
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- Synthesis and biological activity of 2,4-di- p -phenolyl-6- 2 -furanyl-pyridine as a potent topoisomerase II poison
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Dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives were simply achieved using Claisen-Schmidt condensation reaction and modified Kr?hnke pyridine synthetic method. Total forty-five compounds were designed and synthesized which contain hydroxyl groups
- Karki, Radha,Park, Chanmi,Jun, Kyu-Yeon,Kadayat, Tara Man,Lee, Eung-Seok,Kwon, Youngjoo
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p. 360 - 378
(2015/02/19)
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- 4-Fluoro-3′,4′,5′-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model
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Invasion and metastasis are responsible for 90% of cancer-related mortality. Herein, we report on our quest for novel, clinically relevant inhibitors of local invasion, based on a broad screen of natural products in a phenotypic assay. Starting from micromolar chalcone hits, a predictive QSAR model for diaryl propenones was developed, and synthetic analogues with a 100-fold increase in potency were obtained. Two nanomolar hits underwent efficacy validation and eADMET profiling; one compound was shown to increase the survival time in an artificial metastasis model in nude mice. Although the molecular mechanism(s) by which these substances mediate efficacy remain(s) unrevealed, we were able to eliminate the major targets commonly associated with antineoplastic chalcones.
- Roman, Bart I.,De Ryck, Tine,Patronov, Atanas,Slavov, Svetoslav H.,Vanhoecke, Barbara W.A.,Katritzky, Alan R.,Bracke, Marc E.,Stevens, Christian V.
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supporting information
p. 627 - 639
(2015/08/03)
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- Functionalized curcumin analogs as potent modulators of the Wnt/β-catenin signaling pathway
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Osteosarcoma is a primary bone malignancy with aggressive metastatic potential and poor prognosis rates. In our earlier work we have investigated the therapeutic potential of curcumin as an anti-invasive agent in osteosarcoma by its ability to regulate the Wnt/β-catenin signaling pathway. However, the clinical use of curcumin is limited owing to its low potency and poor pharmacokinetic profile. In this study, an attempt was made to achieve more potent Wnt inhibitory activity in osteosarcoma cells by carrying out synthetic chemical modifications of curcumin. We synthesized a total of five series consisting of 43 curcumin analogs and screened in HEK293T cells for inhibition of β-catenin transcriptional activity. Six promising analogs, which were 6.5- to 60-fold more potent than curcumin in inhibiting Wnt activity, were further assessed for their anti-invasive activity and Wnt inhibitory mechanisms. Western blot analysis showed disruption of β-catenin protein nuclear translocation following treatment with analogs 2f, 3c and 4f. Using transwell assays, we also found that these compounds were more potent than 1a (curcumin) in impeding the invasion of osteosarcoma cells, possibly through suppressing MMP-9 activity. Structure-activity-relationship studies revealed that Wnt inhibitory effects could be enhanced by shortening and restraining the flexibility of the 7-carbon linker moiety connecting the terminal aromatic rings of curcumin and substituting both rings with appropriate substituents. Our results demonstrate that the synthesized curcumin analogs are more potent Wnt inhibitors in osteosarcoma cell lines as compared to parental curcumin and are good lead compounds for further development. Future in vivo tests with these compounds will define their therapeutic potentials as promising drug candidates for clinical treatment of osteosarcoma.
- Leow, Pay-Chin,Bahety, Priti,Boon, Choon Pei,Lee, Chong Yew,Tan, Kheng Lin,Yang, Tianming,Ee, Pui-Lai Rachel
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- Nano titania-supported sulfonic acid: An efficient and reusable catalyst for a range of organic reactions under solvent free conditions
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Nano titania-supported sulfonic acid (n-TSA) has been easily prepared from the reaction of nano titania (titanium oxide) with chlorosulfonic acid as sulfonating agent and characterized by the FT-IR spectroscopy, scanning electron microscopy (SEM), X-ray diffraction (XRD) and thermal gravimetric analysis (TGA). The catalytic activity of n-TSA was investigated in the synthesis of important organic derivatives such as pyrimidones, benzothiazoles and chalcones. All of the reactions are very fast and the yields are good to excellent. The catalyst was easily separated and reused for several runs without appreciable loss of its catalytic activity.
- Rahmani, Salman,Amoozadeh, Ali,Kolvari, Eskandar
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p. 184 - 188
(2014/11/08)
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- Discovery of dihydroxylated 2,4-diphenyl-6-thiophen-2-yl-pyridine as a non-intercalative DNA-binding topoisomerase II-specific catalytic inhibitor
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We describe our rationale for designing specific catalytic inhibitors of topoisomerase II (topo II) over topoisomerase I (topo I). Based on 3D-QSAR studies of previously published dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives, 9 novel dihydroxyl
- Jun, Kyu-Yeon,Kwon, Hanbyeol,Park, So-Eun,Lee, Eunyoung,Karki, Radha,Thapa, Pritam,Lee, Jun-Ho,Lee, Eung-Seok,Kwon, Youngjoo
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p. 428 - 438
(2014/05/20)
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- Design and synthesis of 3,5-diaryl-4,5-dihydro-1H-pyrazoles as new tyrosinase inhibitors
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In this study, twenty 3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives with hydroxyl(s) (1a-1p, 2a-2d) were synthesized and their inhibitory activity on mushroom tyrosinase was examined. The results showed that among these compounds, 1-(5-(3,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl) ethanone 1d was found to be the most potent tyrosinase inhibitor with IC 50 value of 0.301 μM. Kinetic study revealed that these compounds were competitive inhibitors of tyrosinase and their structure-activity relationships were investigated in this article.
- Zhou, Zhixuan,Zhuo, Jiaru,Yan, Sujun,Ma, Lin
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p. 2156 - 2162
(2013/05/08)
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- Inhibitory effect of curcumin analogs on tissue factor procoagulant activity and their preliminary structure-activity relationships
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With the aim to explore the multifunctional behaviors of curcumin analogs and to discover new small molecular tissue factor inhibitors, twelve mono carbonyl curcumin analogs of three classes were synthesized and their effect on tissue factor procoagulant activity was evaluated in the human monoblastic leukemia THP-1 cells stimulated by LPS. The most potent compounds 2a exhibited the dramatically enhanced activity with the IC50 values of 0.053 nM. Their preliminary structure-activity relationship was also discussed.
- Ge, Hai-Xia,Chen, Ling,Zhang, Jian,Kou, Jun-Ping,Yu, Bo-Yang
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p. 3242 - 3246
(2013/07/27)
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- Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study
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Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl, or 2- and 4-phenyl rings attached to the central pyridine. They were evaluated for topoisomeras
- Karki, Radha,Thapa, Pritam,Yoo, Han Young,Kadayat, Tara Man,Park, Pil-Hoon,Na, Youngwha,Lee, Eunyoung,Jeon, Kyung-Hwa,Cho, Won-Jea,Choi, Heesung,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 219 - 228
(2012/05/05)
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- Synthesis of norlignans and in vitro inhibitory activity of antigen-induced degranulation
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The synthesis and biological evaluation of a series of novel norlignans are described. Norlignans were evaluated for their inhibitory activity on the release of β-hexosaminidase, a marker of degranulation, from RBL-2H3 cells induced by the IgE-antigen com
- Park, Eonjeong,Yang, Yoon Jung,Kim, Aejin,Kwak, Jong Hwan,Jung, Young Hoon,Kang, Se Chan,Kim, In Su
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supporting information; body text
p. 3653 - 3655
(2012/07/16)
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- Synthesis and topoisomerase II inhibitory and cytotoxic activity of oxiranylmethoxy- and thiiranylmethoxy-chalcone derivatives
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In order to find potential anticancer drug candidate targeting topoisomerases enzyme, we have designed and synthesized oxiranylmethoxy- and thiiranylmethoxy-retrochalcone derivatives and evaluated their pharmacological activity including topoisomerases inhibitory and cytotoxic activity. Of the compounds prepared compound 25 showed comparable or better cytotoxic activity against cancer cell lines tested. Compound 25 inhibited MCF7 (IC50: 0.49 ± 0.21 μM) and HCT15 (IC50: 0.23 ± 0.02 μM) carcinoma cell growth more efficiently than references. In the topoisomerases inhibition test, all the compounds were inactive to topoisomerase I but moderate inhibitors to topoisomerase II enzyme. Especially, compound 25 inhibited topoisomerase II activity with comparable extent to etoposide at 100 μM concentrations. Correlation between cytotoxicity and topoisomerase II inhibitory activity implies that compound 25 can be a possible lead compound for anticancer drug impeding the topoisomerase II function.
- Na, Younghwa,Nam, Jung-Min
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scheme or table
p. 211 - 214
(2011/02/25)
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- Comparative study of conventional and microwave assisted synthesis of chalcones
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An efficient, facile and eco-friendly microwave assisted approach for the synthesis of substituted chalcones by condensation of substituted acetophenones with substituted benzaldehyds in presence of an inorganic base is desired over time consuming convent
- Sharma, Bhavana
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experimental part
p. 2468 - 2470
(2012/01/14)
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- Synthesis and evaluation of some new substituted benzothiazepine and benzoxazepine derivatives as anticonvulsant agents
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A new series of 4-(4′-Hydroxyphenyl)-2-(3-substitutedphenyl)-3-(4-substitutedphenylamino methylene)-2,3-dihydro-1,5-benzothiazepines (3a-3j) and 4-(4′-Hydroxyphenyl)-2-(3-substituted phenyl)-3-(4-substitutedphenylaminomethylene)-2,3-dihydro-1,5-benzoxazep
- Garg, Neha,Chandra, Trilok,Archana,Jain, Amit B.,Kumar, Ashok
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experimental part
p. 1529 - 1535
(2010/06/14)
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- Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone
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The 4′-(p-toluenesulfonylamino)-4-hydroxychalcone (TSAHC), which bears inhibitory chemotypes for both α-glucosidase and tyrosinase, was evaluated for tyrosinase activity and depigmenting ability relative to compounds designed to only target tyrosianse act
- Seo, Woo Duck,Ryu, Young Bae,Curtis-Long, Marcus J.,Lee, Chan Woo,Ryu, Hyung Won,Jang, Ki Chang,Park, Ki Hun
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experimental part
p. 2010 - 2017
(2010/07/04)
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- NaOAc-mediated selective deprotection of aromatic acetates and Its application in the synthesis of natural products
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We have developed an efficient method to deacetylate the aromatic acetates using NaOAc in excellent yields and demonstrated the application of the procedure in the synthesis of natural products.
- Narender,Reddy, K. Papi,Madhur
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experimental part
p. 1949 - 1956
(2009/10/17)
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- Pyrazoline-based mycobactin analogues as MAO-inhibitors
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3,5-Diaryl carbothioamide pyrazolines designed as mycobactin analogs (mycobacterial siderophore) were reported to be potent antitubercular agents under iron limiting condition in our earlier study. Clinical complications of newly introduced antibiotic Linezolid, due its MAO inhibitory activity, prompted us to evaluate our compounds for their MAO-inhibitory activity against rat liver MAO-A and MAO-B as pyrazolines were reported to be antidepressants and MAO inhibitors. The present study carried out with this pilot library of 32 compounds will provide us with necessary information for designing antitubercular molecules with reduced MAO-inhibitory activity and also help us in identifying a selective MAO-B inhibitor which has potential clinical utility in neurodegenerative disorders. Thirty-two compounds analyzed has shown spectrum of activity from selective to nonselective against two isoforms of rat liver MAO-A and MAO-B and also as competitive, reversible to non-competitive, irreversible. It is also interesting to note that anti-tubercular compound 11, 14 and 16 were also found to be selective inhibitors of rat liver MAO-B. Docking studies with human MAO shows that compound 11 interacts with the catalytic site of both the isoforms, suggesting compound 11 as nonselective inhibitor of human MAO isoforms.
- Jayaprakash, Venkatesan,Sinha, Barij N.,Ucar, Gulberk,Ercan, Ayse
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scheme or table
p. 6362 - 6368
(2009/09/30)
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- Liquid crystalline epoxy thermosets
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Rigid rod epoxy compounds can be cured in liquid crystalline structure. The so obtained networks exhibit better mechanical properties with respect to the isotropic ones. The mesogenic character of the epoxy compounds appears more crucial than the molecular geometry of the curing agent in developing liquid crystallinity. The curing temperature plays an important role in affecting the state of order of the thermosets.
- Giamberini,Amendola,Carfagna
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- Microwave-assisted Deacetylation on Alumina: a Simple Deprotection Method
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A simple high-yielding method for the deprotection of acetylated phenols and alcohols is described which occurs under mild conditions on an alumina surface using microwave irradiation.
- Varma, Rajender S.,Varma, Manju,Chatterjee, Arnab K.
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p. 999 - 1000
(2007/10/02)
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- SYNTHESIS OF LIQUID CRYSTALLINE 3,5-DIARYL 1,2-DITHIOLIUM SALTS
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The title compounds are obtained by heterocyclisation of dialkoxy substituted diaryl β-diketones or chalcones using P4S10.
- Veber, M.,Jallabert, C.,Strzeleska, H.
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p. 693 - 702
(2007/10/02)
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