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Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

Title: Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

Authors: Thapa P.; Karki R.; Choi H.; Choi J.H.; Yun M.; Jeong B.-S.; Jung M.-J.; Nam J.M.; Na Y.; Cho W.-J.; Kwon Y.; Lee E.-S.

Ewha Authors: 권영주

SCOPUS Author ID: 권영주

Issue Date: 2010

Journal Title: Bioorganic and Medicinal Chemistry

ISSN: 0968-0896

Citation: Bioorganic and Medicinal Chemistry vol. 18, no. 6, pp. 2245 - 2254

Indexed: SCI; SCIE; SCOPUS

Document Type: Article

Abstract: A series of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives were designed, synthesized, and evaluated for their topoisomerase I and II inhibition and cytotoxic activity against several human cancer cell lines. Compounds 10-19 showed moderate topoisomerase I and II inhibitory activity and 20-29 showed significant topoisomerase II inhibitory activity. Structure-activity relationship study revealed that 4-(5-chlorofuran-2-yl)-2-(thiophen-3-yl) moiety has an important role in displaying topoisomerase II inhibition. © 2010 Elsevier Ltd. All rights reserved.