Article
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M.
Journal of enzyme inhibition and medicinal chemistry - 1 Dec 2022
Gaber Ahmed A, Sobhy Mohamed, Turky Abdallah, Abdulwahab Hanan Gaber, Al-Karmalawy Ahmed A, Elhendawy Mostafa A, Radwan Mohamed M, Elkaeed Eslam B, Ibrahim Ibrahim M, Elzahabi Heba S A, Eissa Ibrahim H
Abstract excerpt
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...
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