Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol

MayhoubA.S.; MarlerL.; KondratyukT.P.ParkE.-J.PezzutoJ.M.CushmanM.

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Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol

机译：Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol

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Aromatase is an established target not only for breast cancer chemotherapy, but also for breast cancer chemoprevention. The moderate and non-selective aromatase inhibitory activity of resveratrol (1) was improved about 100-fold by replacement of the ethylenic bridge with a thiadiazole and the phenyl rings with pyridines (e.g., compound 3). The aromatase inhibitory activity was enhanced over 6000-fold by using a 1,3-thiazole as the central ring and modifying the substituents on the 'A' ring to target the Met374 residue of aromatase. On the other hand, targeting the hydroxyl group of Thr310 by a hydrogen-bond acceptor on the 'B' ring did not improve the aromatase inhibitory activity.

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《Bioorganic and medicinal chemistry》 |2012年第7期|2427-2434|共8页
作者
MayhoubA.S.; MarlerL.; KondratyukT.P.ParkE.-J.PezzutoJ.M.CushmanM.;
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作者单位

College of Pharmacy, University of Hawaii at Hilo, Hilo, HI 96720, United States;

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Aromatase; Chemoprevention; Chemotherapy; Inhibitor; Resveratrol;

Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol

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