4.7 Article

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

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JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 8, 页码 3076-3080

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AMER CHEMICAL SOC
DOI: 10.1021/jm101027s

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  1. National Health Research Institutes
  2. National Science Council, Taiwan, ROC [NSC-95-2113-M-400-001-MY3]

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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%).

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