- Flavone inspired discovery of benzylidenebenzofuran-3(2H)-ones (aurones) as potent inhibitors of human protein kinase CK2
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In this work, we describe the design, synthesis and SAR studies of 2-benzylidenebenzofuran-3-ones (aurones), a new family of potent inhibitors of CK2. A series of aurones have been synthesized. These compounds are structurally related to the synthetic flavones and showed nanomolar activities towards CK2. Biochemical tests revealed that 20 newly synthesized compounds inhibited CK2 with IC50 values in the nanomolar range. Further property-based optimization of aurones was performed, yielding a series of CK2 inhibitors with enhanced lipophilic efficiency. The most potent compound 12m (BFO13) has CLipE = 4.94 (CLogP = 3.5; IC50 = 3.6 nM) commensurable with the best known inhibitors of CK2.
- Bdzhola, V. G.,Bilokin, Y. V.,Borysenko, I. P.,Lukashov, S. S.,Protopopov, M. V.,Prykhod'ko, A. O.,Starosyla, S. A.,Vdovin, V. S.,Yarmoluk, S. M.
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- Aurones as new porcine pancreatic α-amylase inhibitors
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Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturally-occurring structural isomers of flavones, with promising pharmacological potential. Methods: In this study, the structural requirements for the inhibition of porcine pancreatic α-amylase by hydroxylated or methoxylated aurone derivatives were investigated by assessing their in vitro biological activities against porcine pancreatic α-amylase. Results: The structure-activity relationship of these inhibitors based on both in vitro and in silico findings showed that the hydrogen bonds between the OH groups of the A or B ring of (Z)-benzylidenebenzofuran-3-one derivatives and the catalytic residues of the binding site are crucial for their inhibitory activities. Conclusion: It seems that the OH groups in aurones inhibit α-amylase in a manner similar to that of OH groups in flavones and flavonols.
- Roshanzamir, Khashayar,Kashani-Amin, Elaheh,Ebrahim-Habibi, Azadeh,Navidpour, Latifeh
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p. 333 - 340
(2019/06/20)
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- Synthesis of novel pyrazole derivatives and their tumor cell growth inhibitory activity
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To find novel antitumor agents, a series of 1H-benzofuro[3,2-c]pyrazole derivatives 4a-e were designed and synthesized. The treatment of 6-methoxybenzofuran-3(2H)-one 3 with LiHMDS in anhydrous tetrahydrofuran (THF) followed by reaction with 3-substitued phenyl isothiocyanate gave the thioamide intermediates, which underwent condensation with hydrazine monohydrate in dioxane/EtOH (1:1) to provide the benzofuropyrazole derivatives 4a–e as well as the unexpected pyrazole derivatives 5a–e. In tumor cell growth inhibitory assay, all the benzofuropyrazole derivatives were not active against the breast tumor MCF-7 cell, only 4a was highly active and more potent than ABT-751 against the leukemia K562 (GI50 = 0.26 μM) and lung tumor A549 cells (GI50 = 0.19 μM), while other benzofuropyrazoles showed very weak inhibitory activity. In contrast, the pyrazoles 5a-e were in general more potent than the benzofuropyrazoles 4a–e. Compound 5a exhibited a similar tendency to that of 4a with high potency against K562 and A549 cells but weak effects on MCF-7 cell. Both pyrazoles 5b and 5e exhibited high inhibitory activities against K562, MCF-7 and A549 cells. The most active compound 5b was much more potent than ABT-751 against K562 and A549 cells with GI50 values of 0.021 and 0.69 M, respectively. Moreover, 5b was identified as a novel tubulin polymerization inhibitor with an IC50 of 7.30 M.
- Cui, Ying-Jie,Tang, Long-Qian,Zhang, Cheng-Mei,Liu, Zhao-Peng
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- Tryptophan compound, preparation method and application thereof
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The invention relates to a tryptophan compound, a preparation method and application thereof. The molecular formula is (Z)-(2-((2-(4-methoxybenzylidene)-3-oxo-2, 3-dihydrobenzofuran-6-yl)oxyl)acetyl)-D-tryptophan. The small molecule compound has a chiral center, and the absolute configuration is R configuration; the small molecule compound can reach a good inhibitory effect on thrombin, also has low toxicity, good druggability, and good medicinal potential, and provides a new potential option for clinical medication.
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- PD-1/PD-L1 small-molecule inhibitor and preparation method and application thereof
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The invention discloses a PD-1/PD-L1 small-molecule inhibitor and a preparation method and application thereof. Specifically, the invention discloses a compound with the structure shown in the formulaL, a stereoisomer or a tautomer thereof, or pharmaceutically acceptable salts or hydrates or solvates thereof, and please see the specification for specific definitions. The compound has excellent effects for restraining PD-1/PD-L1. Please see the specification for the formula.
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Paragraph 0221; 0226; 0227; 0228
(2019/05/08)
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- Drug design, synthesis and in vitro evaluation of substituted benzofurans as hsp90 inhibitors
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Background: Heat shock protein 90 is a molecular chaperone required for the stability and function of several client proteins that promote cancer cell growth and/or survival. Discovery of Hsp90 inhibitors has emerged as an attractive target of research in cancer therapeutics. Natural products like geldanamycin and radicicol are established Hsp90 inhibitors, but face limitations with toxicity and inactivity, by in vivo studies respectively. However, they lay the logical starting point for the design of novel synthetic or semi-synthetic congeners as Hsp90 inhibitors. Objective: In this article, the structure based drug design of substituted 2-aryl/heteroarylidene-6- hydroxybenzofuran-3(2H)-one analogues to optimize and mimic the pharmacophoric interactions of the valid Hsp90 inhibitor radicicolis focused. Method: In silico docking study was performed by Surflex dock-Geom (SYBYL- X 1.2 drug discovery suite) and the designed ligands were chemically synthesized by conventional method using resorcinol and chlororesorcinol as starting materials. Two dimensional chemical similarity search was carried out to identify the chemical space of 'SY' series in comparison with reported Hsp90 inhibitors. The in vitro cell proliferation assay (resazurin reduction method) and proteomic investigation (DARTS) was carried out on whole cell lysate to evaluate anticancer activity. Results: The chemical structures of all the synthesized compounds were confirmed by IR, 1H-NMR and Mass spectral analysis. The results of chemical similarity search show that SY series fit it in the chemical space defined by existing Hsp90 inhibitors. In vitro cell proliferation assay, against human melanoma and breast cancer cell lines, identified 'SY3' as the promising anticancer agent amongst the series. Conclusion: Docking studies, 2D chemical similarity search, resazurin reduction assay and qualitative proteomic analysis identify 'SY3'as a promising Hsp90 inhibitor amongst the series.
- Kadasi, Sundeep,Costa, Thadeu E.M.M.,Arukala, Neha,Toshakani, Mallika,Duggineti, Chaitanya,Thota, Sreekanth,Gupta, Sayan D.,Raj, Shiva,Penido, Carmen,Henriques, Maria G.,Raghavendra, Nulgumnalli M.
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- Synthesis of 6-hydroxyaurone analogues and evaluation of their α-glucosidase inhibitory and glucose consumption-promoting activity: Development of highly active 5,6-disubstituted derivatives
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A series of 6-hydroxyaurones and their analogues have been synthesized and evaluated for their in vitro α-glucosidase inhibitory and glucose consumption-promoting activity. These compounds exhibited varying degrees of α-glucosidase inhibitory activity, 11 of them showing higher potency than that of the control standard acarbose (IC50?=?50.30?μM). Surprisingly, analogues devoid of a substituent at C-2 but having an aryl group at C-5 were found to be highly active (e.g., 7f, IC50?=?9.88?μM). Docking analysis substantiated these findings. The kinetic analysis of compound 7f, the most potent α-glucosidase inhibitor of this study, revealed that it inhibited α-glucosidase in an irreversible and mixed competitive mode. In addition, compounds 7f and 10c exhibited significant glucose consumption promoting activity at 1?μM.
- Sun, Hua,Ding, Weina,Song, Xiaotong,Wang, Dong,Chen, Mingzhu,Wang, Kaili,Zhang, Yazhou,Yuan, Peng,Ma, Ying,Wang, Runling,Dodd, Robert H.,Zhang, Yongmin,Lu, Kui,Yu, Peng
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supporting information
p. 3226 - 3230
(2017/07/07)
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- Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet β-cells from apoptosis
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Death-associated protein kinase-related apoptosis-inducing kinase-2 (DRAK2) is a serine/threonine kinase that plays a key role in a wide variety of cell death signaling pathways. Inhibition of DRAK2 was found to efficiently protect islet β-cells from apoptosis and hence DRAK2 inhibitors represent a promising therapeutic strategy for the treatment of diabetes. Only very few chemical entities targeting DRAK2 are currently known. We carried out a high throughput screening and identified compound 4 as a moderate DRAK2 inhibitor with an IC50value of 3.15?μM. Subsequent SAR studies of hit compound 4 led to the development of novel benzofuran-3(2H)-one series of DRAK2 inhibitors with improved potency and favorable selectivity profiles against 26 selected kinases. Importantly, most potent compounds 40 (IC50?=?0.33?μM) and 41 (IC50?=?0.25?μM) were found to protect islet β-cells from apoptosis in dose-dependent manners. These data support the notion that small molecule inhibitors of DRAK2 represents a promising strategy for the treatment of diabetes.
- Wang, Sheng,Xu, Lei,Lu, Yu-Ting,Liu, Yu-Fei,Han, Bing,Liu, Ting,Tang, Jie,Li, Jia,Wu, Jiangping,Li, Jing-Ya,Yu, Li-Fang,Yang, Fan
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p. 195 - 208
(2017/03/02)
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- Synthesis and antiproliferative activity of 2-arylidene 6-(2-aryl-2-oxoethoxy)benzofuran-3-one derivatives
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The synthesis of 2-arylidene 6-(2-aryl-2-oxoethoxy)benzofuran-3-one derivatives was reported and selected compounds were determined for their anticancer activity evaluation in National Cancer Institute NCI, USA according to the drug screening protocol of the institute against approximately 60 tumor cell lines derived from nine cancer diseases. Compound 3r, namely 2-(4-chlorobenzylidene)-6-[2-(4-methoxyphenyl)-2-oxoethoxy]benzofuran-3-one exhibited the highest antitumor activity against non-small lung cancer cell lines.
- Demirayak, Seref,Yurttas, Leyla,Karaburun, Ahmet Cagri,Gundogdu-Karaburun, Nalan,Kayagil, Ismail
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p. 563 - 569
(2016/07/19)
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- Blood-brain barrier permeable anticholinesterase aurones: Synthesis, structure-activity relationship, and drug-like properties
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A series of novel aurones bearing amine and carbamate functionalities at various positions (rings A and/or B) of the scaffold was synthesized and evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activities. Structure-activity relationship study disclosed several potent submicromolar acetylcholinesterase inhibitors (AChEIs) particularly aurones bearing piperidine and pyrrolidine moieties at ring A or ring B. Bulky groups particularly methoxyls, and carbamate to a lesser extent, at either rings were also prominently featured in these AChEI aurones as exemplified by the trimethoxyaurone 4-3. The active aurones exhibited a lower butyrylcholinesterase inhibition. A 3g€2-chloroaurone 6-3 originally designed to improve the metabolic stability of the scaffold was the most potent of the series. Molecular docking simulations showed these AChEI aurones to adopt favourable binding modes within the active site gorge of the Torpedo californica AChE (TcAChE) including an unusual chlorine-π interaction by the chlorine of 6-3 to establish additional bondings to hydrophobic residues of TcAChE. Evaluation of the potent aurones for their blood-brain barrier (BBB) permeability and metabolic stability using PAMPA-BBB assay and in vitro rat liver microsomes (RLM) identified 4-3 as an aurone with an optimal combination of high passive BBB permeability and moderate CYP450 metabolic stability. LC-MS identification of a mono-hydroxylated metabolite found in the RLM incubation of 4-3 provided an impetus for further improvement of the compound. Thus, 4-3, discovered within this present series is a promising, drug-like lead for the development of the aurones as potential multipotent agents for Alzheimer's disease.
- Liew, Kok-Fui,Chan, Kit-Lam,Lee, Chong-Yew
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p. 195 - 210
(2015/03/18)
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- 2-Diazo-1-(4-hydroxyphenyl)ethanone: A versatile photochemical and synthetic reagent
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α-Diazo arylketones are well-known substrates for Wolff rearrangement to phenylacetic acids through a ketene intermediate by either thermal or photochemical activation. Likewise, α-substituted p-hydroxyphenacyl (pHP) esters are substrates for photo-Favorskii rearrangements to phenylacetic acids by a different pathway that purportedly involves a cyclopropanone intermediate. In this paper, we show that the photolysis of a series of α-diazo-p- hydroxyacetophenones and p-hydroxyphenacyl (pHP) α-esters both generate the identical rearranged phenylacetates as major products. Since α-diazo-p-hydroxyacetophenone (1a, pHP N2) contains all the necessary functionalities for either Wolff or Favorskii rearrangement, we were prompted to probe this intriguing mechanistic dichotomy under conditions favorable to the photo-Favorskii rearrangement, i.e., photolysis in hydroxylic media. An investigation of the mechanism for conversion of 1a to p-hydroxyphenyl acetic acid (4a) using time-resolved infrared (TRIR) spectroscopy clearly demonstrates the formation of a ketene intermediate that is subsequently trapped by solvent or nucleophiles. The photoreaction of 1a is quenched by oxygen and sensitized by triplet sensitizers and the quantum yields for 1a-c range from 0.19 to a robust 0.25. The lifetime of the triplet, determined by Stern-Volmer quenching, is 31 ns with a rate for appearance of 4a of k = 7.1 × 10 6 s-1 in aq. acetonitrile (1:1 v:v). These studies establish that the primary rearrangement pathway for 1a involves ketene formation in accordance with the photo-Wolff rearrangement. Furthermore we have also demonstrated the synthetic utility of 1a as an esterification and etherification reagent with a variety of substituted α-diazo-p- hydroxyacetophenones, using them as synthons for efficiently coupling it to acids and phenols to produce pHP protect substrates. The Royal Society of Chemistry and Owner Societies.
- Senadheera, Sanjeewa N.,Evans, Anthony S.,Toscano, John P.,Givens, Richard S.
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p. 324 - 341
(2014/02/14)
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- Synthetic models related to methoxalen and menthofuran-cytochrome P450 (CYP) 2A6 interactions. Benzofuran and coumarin derivatives as potent and selective inhibitors of CYP2A6
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Human microsomal cytochrome P450 (CYP) 2A6 contributes extensively to nicotine detoxication but also activates tobacco-specific procarcinogens to mutagenic products. We prepared a series of benzofuran and coumarin derivatives that have inhibitory effects on the activity of human CYP2A6. The reported compounds methoxalen and menthofuran had potent inhibitory effects on the activity of CYP2A6 with IC50 values of 0.47 μM and 1.27 μM, respectively. Synthetic benzofuran (4-methoxybenzofuran: IC50=2.20 μM) and coumarin (5-methoxycoumarin: IC50=0.13 μM and 6-methoxycoumarin: IC50=0.64 μM) derivatives, which have more selective effects than those of methoxalen and menthofuran, exhibited comparable activities against CYP2A6. These compounds can be used as a lead compounds in the design of CYP2A6 inhibitor drugs to reduce smoking and tobacco-related cancers.
- Yamaguchi, Yuki,Akimoto, Ichie,Motegi, Kyoko,Yoshimura, Teruki,Wada, Keiji,Nishizono, Naozumi,Oda, Kazuaki
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p. 997 - 1001
(2013/11/19)
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- Synthesis and structural characterization of 2-benzylidenebenzofuran-3-(2 H)-ones
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Novel aurone derivatives e.g. 2-(2-(3-methylbut-2-enyloxy)benzylidene) benzofuran-3(2H)-one (3a), 2-(2-(allyloxy)benzylidene)-7-methoxybenzofuran-3(2H) -one (3b), and 2-(5-bromo-2-(3-methylbut-2-enyloxy)benzylidene)-6- hydroxybenzofuran-3(2H)-one (3c) were synthesized. All these compounds were characterized by IR, 1H and 13C NMR, and Mass spectroscopy. Finally, the crystal structures were solved by single crystal X-ray diffraction data and the structures were analyzed in terms of supramolecular interactions. [Supplementary materials are available for this article. Go to the publisher's online edition of Molecular Crystals and Liquid Crystals for the following free supplemental resource(s): supplemental figures 1-12; Spectral data (IR, NMR, MS, and HRMS) of the compounds 3a, 3b and 3c are available in the supporting information in.pdf format. Crystallographic information files (.cif) of compounds 3a, 3b, and 3c are available in the electronic format.]
- Rambabu,Srinivas,Manjulatha, Khanapur,Basavoju, Srinivas,Basaveswara Rao,Pal, Manojit
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- Synthesis and in vitro characterization of some benzothiazole- and benzofuranone-derivatives for quantification of fibrillar aggregates and inhibition of amyloid-mediated peroxidase activity
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Neurodegenerative diseases are characterized by amyloid deposition. Thioflavin T (ThT) is one of the molecules considered for detection of amyloid deposits; however, its lipophilicity is too low to cross the blood-brain barrier. Therefore, there is a strong motivation to develop suitable compounds for in vitro fibril quantification as well as for in vivo amyloid imaging. Moreover, oxidative stress (particularly, uncontrolled peroxidase activity) has frequently been reported to play a critical role in the onset/progression of some neurodegenerative disorders. In this study, we describe the synthesis of some benzothiazole and benzofuranone compounds and examine their peroxidase inhibitory properties. Furthermore, to establish the potential binding of synthesized compounds to amyloid aggregates, their in vitro binding to some non-disease related amyloidogenic proteins were characterized. Analyses of the in vitro binding studies indicated that compounds 2 and 4 bind to the amyloid structures successfully while compounds 1 and 3 showed a low affinity in binding to fibrils. Furthermore, compounds 3 and 4 were observed to inhibit amyloid-mediated peroxidase activity in a reversible un-competitive manner.
- Ghadami, Seyyed Abolghasem,Hossein-Pour, Zahra,Khodarahmi, Reza,Ghobadi, Sirous,Adibi, Hadi
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p. 115 - 126
(2013/03/14)
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- Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase
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A novel series of coumarin and 3-coumaranone derivatives encompassing the phenacyl pyridinium moiety were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity using Ellman's method. All compounds presented inhibitory activity against both AChE and BuChE in the micromolar range. The molecular docking simulations revealed that all compounds were dual binding site inhibitors of AChE. A kinetic study was performed and the mechanism of enzyme inhibition was proved to be of mixed type. All compounds were tested for their antioxidant activity and no significant activity was observed.
- Alipour, Masoumeh,Khoobi, Mehdi,Nadri, Hamid,Sakhteman, Amirhossein,Moradi, Alireza,Ghandi, Mehdi,Foroumadi, Alireza,Shafiee, Abbas
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p. 577 - 587
(2013/09/02)
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- Discovery of naturally occurring aurones that are potent allosteric inhibitors of hepatitis C virus RNA-dependent RNA polymerase
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We have identified naturally occurring 2-benzylidenebenzofuran-3-ones (aurones) as new templates for non-nucleoside hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors. The aurone target site, identified by site-directed mutagenesis, is located in thumb pocket I of HCV RdRp. The RdRp inhibitory activity of 42 aurones was rationally explored in an enzyme assay. Molecular docking studies were used to determine how aurones bind to HCV RdRp and to predict their range of inhibitory activity. Seven aurone derivatives were found to have potent inhibitory effects on HCV RdRp, with IC50 below 5 μM and excellent selectivity index (inhibition activity versus cellular cytotoxicity). The most active aurone analogue was (Z)-2-((1-butyl-1H-indol-3-yl)methylene)-4,6-dihydroxybenzofuran-3(2H)-one (compound 51), with an IC50 of 2.2 μM. Their potent RdRp inhibitory activity and their low toxicity make these molecules attractive candidates as direct-acting anti-HCV agents.
- Haudecoeur, Romain,Ahmed-Belkacem, Abdelhakim,Yi, Wei,Fortuné, Antoine,Brillet, Rozenn,Belle, Catherine,Nicolle, Edwige,Pallier, Coralie,Pawlotsky, Jean-Michel,Boumendjel, Ahcène
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p. 5395 - 5402
(2011/10/02)
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- Specificity of Calreticulin Transacetylase to acetoxy derivatives of benzofurans: Effect on the activation of platelet Nitric Oxide Synthase
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Calreticulin Transacetylase (CRTAase) catalyzes the transfer of acetyl group(s) from polyphenolic acetates (PAs) to functional proteins, such as Glutathione S-transferase (GST), NADPH Cytochrome c reductase and Nitric Oxide Synthase (NOS) resulting in the modulation of biological activities. A comparison of the specificities of the acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones has been carried out earlier by us with an aim to study the effect of nature and position of the acetoxy groups on the benzenoid ring and the position of the carbonyl group with respect to oxygen/nitrogen heteroatom for the catalytic activity of CRTAase. In this communication for the first time, we have studied the influence of differently substituted benzofurans on the CRTAase activity to study the effect of the replacement of pyran ring of coumarin with furan ring, presence of carbonyl at C-3, substitution of C-3 carbonyl group with acetoxy group and presence of various substituents (OAc/OH/Cl) on the benzenoid ring. It was observed that acetoxy derivatives of benzofurans lead to inhibition of ADP induced platelet aggregation by the activation of platelet Nitric Oxide Synthase catalyzed by CRTAase. Accordingly, the formation of NO in platelets by 3-oxo-2,3-dihydrobenzofuran-6,7-diyl diacetate (3a) was found to be comparable with that of model polyphenolic acetate (PA), 7,8-diacetoxy-4-methylcoumarin (DAMC).
- Gupta, Anjali,Priya, Nivedita,Jalal, Sarah,Singh, Prabhjot,Chand, Karam,Raj, Hanumantharao G.,Parmar, Virinder S.,DePass, Anthony L.,Sharma, Sunil K.
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p. 1180 - 1185
(2011/11/06)
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- Functionalized aurones as inducers of NAD(P)H:quinone oxidoreductase 1 that activate AhR/XRE and Nrf2/ARE signaling pathways: Synthesis, evaluation and SAR
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The chemopreventive potential of functionalized aurones and related compounds as inducers of NAD(P)H:quinone oxidoreductase 1 (NQO1, EC 1.6.99.2) are described. Several 4,6-dimethoxy and 5-hydroxyaurones induced NQO1 activity of Hepa1c1c7 cells by 2-fold at submicromolar concentrations, making these the most potent inducers to be identified from this class. Mechanistically, induction of NQO1 was mediated by the activation of AhR/XRE and Nrf2/ARE pathways, indicating that aurones may be mixed activators of NQO1 induction or agents capable of exploiting the proposed cross-talk between the AhR and Nrf2 gene batteries. QSAR analysis by partial least squares projection to latent structures (PLS) identified size parameters, in particular those associated with non-polar surface areas, as an important determinant of induction activity. These were largely determined by the substitution on rings A and B. A stereoelectronic role for the exocyclic double bond as reflected in the E LUMO term was also identified. The electrophilicity of the double bond or its effect on the conformation of the target compound are possible key features for induction activity.
- Lee, Chong-Yew,Chew, Eng-Hui,Go, Mei-Lin
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experimental part
p. 2957 - 2971
(2010/09/03)
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- Design, synthesis and anticholinesterase activity of a novel series of 1-benzyl-4-((6-alkoxy-3-oxobenzofuran-2(3H)-ylidene) methyl) pyridinium derivatives
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A novel series of benzofuranone-ylidene-methyl benzylpyridinium derivatives (6a-u) were synthesized as acetylcholinesterase inhibitors. The anticholinesterase activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that some synthesized compounds exhibited high anticholinesterase activity, among them compound 6b was the most active compound (IC50 = 10 ± 6.87 nM).
- Nadri, Hamid,Pirali-Hamedani, Morteza,Shekarchi, Maryam,Abdollahi, Mohammad,Sheibani, Vahid,Amanlou, Massoud,Shafiee, Abbas,Foroumadi, Alireza
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scheme or table
p. 6360 - 6366
(2010/10/01)
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- ANTIDIABETIC BICYCLIC COMPOUNDS
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Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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Page/Page column 12
(2008/06/13)
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- A method of cosmetic depigmentation care by applying at least one aurone
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At least one aurone or a natural or synthetic derivative of aurone, or an analogue of aurone, in which the independent phenyl ring can be substituted by a heterocycle of pyrrole, imidazole, triazole, pyridine, furan, or thiophene type, is disclosed as a cosmetic agent, or as an active substance, for the manufacture either of a cosmetic composition, or of a pharmaceutical composition, notably a dermatological composition, having a melanogenesis-inhibiting activity or a depigmenting activity, or an anti-tyrosinase activity.
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Page/Page column 9
(2008/06/13)
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- Synthesis and anticancer effect of B-ring trifluoromethylated flavonoids
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A series of B-ring trifluoromethylated flavonoids derivatives were prepared and tested in vitro against human gastric adenocarcinoma cell line (SGC-7901). Among these derivatives, 5,7-dipropoxy-2-(4′ -trifluoromethylphenyl)-chromen-4-one 5c had the strongest activity against SGC-7901 cell.
- Zheng, Xing,Cao, Jian-Guo,Meng, Wei-Dong,Qing, Feng-Ling
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p. 3423 - 3427
(2007/10/03)
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- Synthesis of acid addition salts of hydroxylamines
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This invention relates to novel diastereomeric acid addition salts of homochiral hydroxylamines, to processes for obtaining such, to processes for the conversion thereof to the corresponding homochiral hydroxylamines, to certain novel homochiral hydroxylamines and the processes for using these as intermediates.
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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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- Studies on Pitch Problems Caused by Pulping and Bleaching of Tropical Woods. XIV. Chemistry of the Aurone Derivatives at the Conventional Bleaching Stages
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Rengasin (1), which is responsible for the colored specks on a sheet of bleached sulfate pulp from the woods of rengas (Anacardiaceae), was converted into R1 7 having a novel carbon skeleton.A closely related analogue, S1 8, prepared from sulfuretin (2) was used as a model to investigate further conversions under bleaching conditions.Chlorination of S1 8 produced an equilibrium mixture involving compound 9 as a dominant compound.The latter was transformed by the treatment with chlorine dioxide into an orthoquinone (16) via two pathway containing 10 in one and 15 in another.The monomeric quinone (16) immediately dimerized in acidic media to give 20 under the same conditions as above, and the further oligomerization by the process similar to that in dimerization of 16 finally afforded a mixture of colored oligomers 26.
- Ohtani, Yoshito,Sumimoto, Masashi
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p. 613 - 622
(2007/10/02)
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- Carbon-13 Nmr Spectroscopy of Methoxy- and Acetoxyaurones
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The 13C nmr chemical shifts of methoxy and acetoxyaurones are reported.The signals are assigned on the basis of substituent effects and comaprison with structurally related compounds.Assignments are also verified by Sford.
- Sharma, Anil,Chibber, S. S.
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p. 275 - 277
(2007/10/02)
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