| 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 |
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