Scaffold-hopping strategy: synthesis and biological evaluation of 5, 6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents

…, JY Chang, JP Liou, P Shukla, CW Chang…

Index: Tung, Yen-Shih; Coumar, Mohane Selvaraj; Wu, Yu-Shan; Shiao, Hui-Yi; Chang, Jang-Yang; Liou, Jing-Ping; Shukla, Paritosh; Chang, Chun-Wei; Chang, Chi-Yen; Kuo, Ching-Chuan; Yeh, Teng-Kuang; Lin, Chin-Yu; Wu, Jian-Sung; Wu, Su-Ying; Liao, Chun-Chen; Hsieh, Hsing-Pang Journal of Medicinal Chemistry, 2011 , vol. 54, # 8 p. 3076 - 3080

Full Text: HTML

Citation Number: 35

Abstract

Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5, 6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shuffling of the nitrogen from the N-1 position or by insertion of one or two nitrogen atoms into the indole core of 1. Among these, 7-azaindole core 12 showed potent in vitro anticancer activity and ...