Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFR^WT and EGFR^T790M.

ABSTRACT: New 1H-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesised to act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives were assessed for their in vitro anti-proliferative activities against A549 and HCT-116 cancer cells. Compounds 8, 10, 12a, and 12b showed potent anti-proliferative activities. Compound 12b was the most promising member with IC₅₀ values of 8.21 and 19.56 µM against A549 and HCT-116, respectively. Compounds 8, 10, 12a, and 12b were evaluated for their kinase inhibitory activities against wild EGFR (EGFR^WT). Compound 12b was the most potent member showing an IC₅₀ value of 0.016 µM. In addition, compound 12b showed noticeable activity

SUBMITTER: Gaber AA 

PROVIDER: S-EPMC9466626 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature