@article{b8928d275065429e825511ce956f4d33,
title = "Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents",
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 improved oral bioavailability (F = 35%) compared with 1 (F <10%).",
author = "Tung, {Yen Shih} and Coumar, {Mohane Selvaraj} and Wu, {Yu Shan} and Shiao, {Hui Yi} and Chang, {Jang Yang} and Liou, {Jing Ping} and Paritosh Shukla and Chang, {Chun Wei} and Chang, {Chi Yen} and Kuo, {Ching Chuan} and Yeh, {Teng Kuang} and Lin, {Chin Yu} and Wu, {Jian Sung} and Wu, {Su Ying} and Liao, {Chun Chen} and Hsieh, {Hsing Pang}",
year = "2011",
month = apr,
day = "28",
doi = "10.1021/jm101027s",
language = "English",
volume = "54",
pages = "3076--3080",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "8",
}