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Design, synthesis and anticancer evaluation of 1H-pyrazolo[3,4-d]pyrimidine derivatives as potent EGFRWT and EGFRT790M inhibitors and apoptosis inducers.

Bioorganic chemistry - 1 Oct 2018

Gaber Ahmed A, Bayoumi Ashraf H, El-Morsy Ahmed M, Sherbiny Farag F, Mehany Ahmed B M, Eissa Ibrahim H

Abstract excerpt

In our attempt to develop effective EGFR-TKIs, two series of 1H-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated in vitro for their inhibitory activities against EGFRWT. Compounds 15b, 15j, and 18d potently inhibited EGFRWT at sub-micro molar IC50 values comparable to that of erlotinib. Moreover, thirteen compounds that showed promising IC50...

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Identifiers

PMID: 29986185
DOI: 10.1016/j.bioorg.2018.06.017

Genes

EGFR

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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