Antitumor agents. 177 1. Design, syntheses, and biological evaluation of novel etoposide analogs bearing pyrrolecarboxamidino group as DNA topoisomerase II …

Z Ji, HK Wang, KF Bastow, XK Zhu, SJ Cho…

Index: Ji, Zheng; Wang, Hui-Kang; Bastow, Kenneth F.; Zhu, Xiao-Kang; Cho, Sung Jin; Cheng, Yung-Chi; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 5 p. 607 - 612

Full Text: HTML

Citation Number: 29

Abstract

Novel water-soluble 4β-amino-4′-O-demethylepipodophyllotoxin derivatives (6–12), designed to enhance minor groove binding ability, were synthesized and screened against NCI's in vitro disease-oriented human tumor cells. Among them, 4′-O-demethyl-4β-[N-(1‴- methyl-4‴-nitro-pyrrole-2‴-carbonyl)-4 ″-aminoanilino]-4-desoxypodophyllotoxin (10) and its HCl salt (11) were found to exhibit potent cytotoxic activities (average log GI50=− 6.91,− ...