Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety.

Abstract

We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Most compounds showed better topoisomerase II inhibitory activity compared to topoisomerase I inhibitory activity. Compounds 19, 20, 26-28, and 47-50 especially showed stronger topo II inhibitory activity than etoposide.

• Authors: Pritam Thapa, Radha Karki, Minho Yun, Tara Man Kadayat, Eunyoung Lee, Han Byeol Kwon, Younghwa Na, Won-Jea Cho, Nam Doo Kim, Byeong-Seon Jeong, Youngjoo Kwon, Eung-Seok Lee
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 52 Pg. 123-36 (Jun 2012) ISSN: 1768-3254 [Electronic] France
• PMID: 22503656 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Masson SAS. All rights reserved.

Chemical References

• Antineoplastic Agents
• Phenols
• Pyridines
• DNA Topoisomerases, Type I
• DNA Topoisomerases, Type II

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Chemistry Techniques, Synthetic
• DNA Topoisomerases, Type I (chemistry, metabolism)
• DNA Topoisomerases, Type II (chemistry, metabolism)
• Drug Design
• Humans
• Models, Molecular
• Phenols (chemistry)
• Protein Conformation
• Pyridines (chemical synthesis, chemistry, pharmacology)