Discovery of New Pyrrolo[2,3-d]pyrimidine Derivatives as Potential Multi-Targeted Kinase Inhibitors and Apoptosis Inducers.

ABSTRACT: In the pursuit of developing more potent and effective targeted kinase inhibitors (TKIs), a series of new compounds, specifically halogenated '(E)-4-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N'-benzylidenebenzohydrazides', were successfully synthesized in three steps with high yields. Among these novel compounds, namely 5e, 5h, 5k, and 5l, promising cytotoxic effects were observed against four different cancer cell lines, with IC₅₀ values ranging from 29 to 59 µM. Notably, compound 5k emerged as the most potent inhibitor, exhibiting significant activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC₅₀ values ranging from 40 to 204 nM, comparable to the well-known TKI sunitinib (IC₅₀ = 261

SUBMITTER: Alotaibi AA 

PROVIDER: S-EPMC10536928 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature