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A new series of 2-phenol-4-aryl-6-chlorophenyl pyridine derivatives as dual topoisomerase I/II inhibitors: Synthesis, biological evaluation and 3D-QSAR study

Title
A new series of 2-phenol-4-aryl-6-chlorophenyl pyridine derivatives as dual topoisomerase I/II inhibitors: Synthesis, biological evaluation and 3D-QSAR study
Authors
Karki, RadhaJun, Kyu-YeonKadayat, Tara ManShin, SominMagar, Til Bahadur ThapaBist, GaneshShrestha, AarajanaNa, YounghwaKwon, YoungjooLee, Eung-Seok
Ewha Authors
권영주전규연
SCOPUS Author ID
권영주scopus
Issue Date
2016
Journal Title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN
0223-5234JCR Link1768-3254JCR Link
Citation
vol. 113, pp. 228 - 245
Keywords
Antitumor agentsCoMFACytotoxicity3D-QSARDual topoisomerase I and II inhibition2-phenol-4-aryl-6-chlorophenyl pyridine
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
As a continuous effort to develop novel antitumor agents, a new series of forty-five 2-phenol-4-aryl-6-chlorophenyl pyridine compounds were synthesized and evaluated for cytotoxicity against four different human cancer cell lines (DU145, HCT15, T47D, and HeLa), and topoisomerase I and II inhibitory activity. Several compounds (10-15, 20, 22, 24, 28, 42, and 49) displayed strong to moderate dual topoisomerase I and II inhibitory activity at 100 mu M. It was observed that hydroxyl and chlorine moiety at meta or para position of phenyl ring is favorable for dual topoisomerase inhibitory activity and cytotoxicity. Most of the compounds displayed stronger cytotoxicities than those of all positive controls against the HCT15 and T47D cell lines. For investigation of the structure-activity relationships, a 3D-QSAR analysis using the method of comparative molecular field analysis (CoMFA) was performed. The generated 3D contour maps can be used for further rational design of novel terpyridine derivatives as highly selective and potent cytotoxic agents. (C) 2016 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2016.02.050
Appears in Collections:
약학대학 > 약학과 > Journal papers
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