Get started
Work

Design and Synthesis of Novel Pyrazolopyrimidine Candidates As Promising EGFR-T790M Inhibitors and Apoptosis Inducers

Year: 2023
Type: article
Abstract: Aim: Our objective was to design and synthesize a new range of pyrazolopyrimidines while maintaining the key pharmacophoric features of EGFR tyrosine kinase inhibitors. Materials & methods: Percentage inhibition in 14 human cancer cell lines and IC50 values were recorded. Compounds 6c, 7e and 7f were examined against both wild and mutant (T790M) EGFR subtypes. Apoptosis markers, cell cycle arrest, apoptosis assay and molecular docking were performed. Results: Compounds 6c, 7e and 7f demonstrated superior inhibitory potentials against wild and mutant (T790M) EGFR subtypes. A molecular docking study showed that compounds 6c and 7e had the best fit. Conclusion: The designed candidates demonstrated superior inhibitory potential as promising EGFR-T790M inhibitors that agrees with the proposed rationale.
DOI: 10.4155/fmc-2023-0156
Authors: Ahmed A Gaber, Marwa Sharaky, Ayman Abo Elmaaty, Mohamed M Hammouda, Ahmed AE Mourad, Samy Y Elkhawaga, Mahmoud Mohamed Mokhtar, Amr S Abouzied, Mai AE Mourad, Ahmed A Al-Karmalawy
Institutions: Al-Azhar University, Cairo University, Port Said University, Prince Sattam Bin Abdulaziz University, Mansoura University, University of Ha'il, National Organization for Drug Control and Research, Horus University – Egypt, Ahram Canadian University
Language: English
Field: Chemistry
Open Access status: green
Award: G188680697
OpenAlex ID: W4387950355
FWCI: 1.07
Cites: 56
Cited by: 11
Related to: 10