2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship
作者:Arjun Basnet、Pritam Thapa、Radha Karki、Younghwa Na、Yurngdong Jahng、Byeong-Seon Jeong、Tae Cheon Jeong、Chong-Soon Lee、Eung-Seok Lee
DOI:10.1016/j.bmc.2007.04.047
日期:2007.7
Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-memberd heteroaromatics as antitumor agents. They were evaluated their topoisomerase I and II inhibitory activities along with cytotoxicities against several human cancer cell lines. Among the prepared compounds, 10-20 showed significant topoisomerase I or II inhibitory activities, and 21-26 showed considerable cytotoxicities against several human cancer cell lines. Structure-activity relationship study indicates that 4-pyridine at 6-position of central pyridine plays a key role in biological activity. (c) 2007 Elsevier Ltd. All rights reserved.