Issue 5, 2024

Pyrazolopyridine-based kinase inhibitors for anti-cancer targeted therapy

Abstract

The need for effective cancer treatments continues to be a challenge for the biomedical research community. In this case, the advent of targeted therapy has significantly improved therapeutic outcomes. Drug discovery and development efforts targeting kinases have resulted in the approval of several small-molecule anti-cancer drugs based on ATP-mimicking heterocyclic cores. Pyrazolopyridines are a group of privileged heterocyclic cores in kinase drug discovery, which are present in several inhibitors that have been developed against various cancers. Notably, selpercatinib, glumetinib, camonsertib and olverembatinib have either received approval or are in late-phase clinical studies. This review presents the success stories employing pyrazolopyridine scaffolds as hinge-binding cores to address various challenges in kinase-targeted drug discovery research.

Graphical abstract: Pyrazolopyridine-based kinase inhibitors for anti-cancer targeted therapy

Article information

Article type
Review Article
Submitted
02 Jan 2024
Accepted
24 Mar 2024
First published
25 Mar 2024

RSC Med. Chem., 2024,15, 1452-1470

Pyrazolopyridine-based kinase inhibitors for anti-cancer targeted therapy

P. Halder, A. Rai, V. Talukdar, P. Das and N. R. Lakkaniga, RSC Med. Chem., 2024, 15, 1452 DOI: 10.1039/D4MD00003J

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