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Current Topics in Medicinal Chemistry

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ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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Review Article

Pyrimidine-fused Dinitrogenous Penta-heterocycles as a Privileged Scaffold for Anti-Cancer Drug Discovery

Author(s): Wen Li, Jinyang Zhang, Min Wang, Ru Dong, Xin Zhou, Xin Zheng and Liping Sun*

Volume 22, Issue 4, 2022

Published on: 11 January, 2022

Page: [284 - 304] Pages: 21

DOI: 10.2174/1568026622666220111143949

Price: $65

Abstract

Pyrimidine-fused derivatives that are the inextricable part of DNA and RNA play a key role in the normal life cycle of cells. Pyrimidine-fused dinitrogenous penta-heterocycles, including pyrazolopyrimidines and imidazopyrimidines are a special class of pyrimidine-fused compounds contributing to an important portion in anti-cancer drug discovery, which has been discovered as the core structure for promising anti-cancer agents used in the clinic or clinical evaluations. Pyrimidinefused dinitrogenous penta-heterocycles have become one privileged scaffold for anti-cancer drug discovery. This review consists of the recent progress of pyrimidine-fused dinitrogenous pentaheterocycles as anti-cancer agents and their synthetic strategies. In addition, this review also summarizes some key structure-activity relationships (SARs) of pyrimidine-fused dinitrogenous pentaheterocycle derivatives as anti-cancer agents.

Keywords: Privileged scaffold, Pyrazolo[1, 5-a]pyrimidines, Pyrazolo[3, 4-b]pyrimidines, Pyrazolo[4, 3-b]pyrimidines, Purines, Imidazo[1, 2-a] pyrimidines, Anti-cancer agents.

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