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一种新型茚并[1,2-b]吡啶酮衍生物，一种DNA嵌入型人拓扑异构酶IIα催化抑制剂，具有不依赖半胱天冬酶3的抗癌活性。

A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity.

作者信息

Jeon K H, Park C, Kadayat T M, Shrestha A, Lee E S, Kwon Y

机构信息

College of Pharmacy, Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.

出版信息

Chem Commun (Camb). 2017 Jun 22;53(51):6864-6867. doi: 10.1039/c7cc02372c.

DOI:10.1039/c7cc02372c
PMID:28604852
Abstract

A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5H-indeno[1,2-b]pyridin-5-one (TI-1-190) was synthesized using a simple microwave-assisted method and its mode of action was systematically characterized. It is a DNA intercalative human topoisomerase IIα catalytic inhibitor with much stronger activity and less DNA toxicity than etoposide, a topoisomerase II poison. TI-1-190 displays caspase 3-independent anticancer activity, unlike etoposide.

摘要

采用简单的微波辅助方法合成了一种新型的2-(呋喃-2-基)-4-(吡啶-2-基)-5H-茚并[1,2-b]吡啶-5-酮(TI-1-190)，并对其作用模式进行了系统表征。它是一种DNA嵌入型人拓扑异构酶IIα催化抑制剂，与拓扑异构酶II毒药依托泊苷相比，具有更强的活性和更低的DNA毒性。与依托泊苷不同，TI-1-190具有不依赖半胱天冬酶3的抗癌活性。

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