Scaffold-Hopping Strategy: Synthesis and Biological Evaluation of 5,6-Fused Bicyclic Heteroaromatics To Identify Orally Bioavailable Anticancer Agents

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DC Field	Value	Language
dc.contributor.author	Shukla, Paritosh	-
dc.date.accessioned	2021-11-11T10:53:50Z	-
dc.date.available	2021-11-11T10:53:50Z	-
dc.date.issued	2011-03-24	-
dc.identifier.uri	https://pubs.acs.org/doi/abs/10.1021/jm101027s	-
dc.identifier.uri	http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/3288	-
dc.description.abstract	Utilizing a 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%).	en_US
dc.language.iso	en	en_US
dc.publisher	ACS	en_US
dc.subject	Chemistry	en_US
dc.subject	Anticancer activity	en_US
dc.subject	Anions	en_US
dc.subject	Scaffolds	en_US
dc.title	Scaffold-Hopping Strategy: Synthesis and Biological Evaluation of 5,6-Fused Bicyclic Heteroaromatics To Identify Orally Bioavailable Anticancer Agents	en_US
dc.type	Article	en_US
Appears in Collections:	Department of Chemistry

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