Synthesis, biological evaluation and molecular modeling study of [1, 2, 4]-Triazolo [4, 3-c] quinazolines: New class of EGFR-TK inhibitors

WA Ewes, MA Elmorsy, SM El-Messery… - Bioorganic & medicinal …, 2020 - Elsevier
Abstract New series of triazolo [4, 3-c] quinazolines were designed, synthesized and their
structures were elucidated using different spectroscopic techniques. They were evaluated …

Novel Pyrazoloquinolin-2-ones: Design, synthesis, docking studies, and biological evaluation as antiproliferative EGFR-TK inhibitors

MAI Elbastawesy, AA Aly, M Ramadan… - Bioorganic …, 2019 - Elsevier
Two new series of diethyl 2-[2-(substituted-2-oxo-1, 2-dihydroquinolin-4-yl) hydrazono]-
succinates 6a-g and 1-(2-oxo-1, 2-dihydroquinolin-4-yl)-1H-pyrazoles 7a-f have been …

New oxadiazole and pyrazoline derivatives as anti-proliferative agents targeting EGFR-TK: design, synthesis, biological evaluation and molecular docking study

MI Serag, SS Tawfik, SMI Badr, HM Eisa - Scientific Reports, 2024 - nature.com
Two new series of oxadiazole and pyrazoline derivatives were designed and synthesized as
promising EGFR-TK inhibitors. The in vitro antiproliferative activity was studied against three …

Design, synthesis, anticancer activity and docking studies of novel quinazoline-based thiazole derivatives as EGFR kinase inhibitors

MS Raghu, HA Swarup, T Shamala, BS Prathibha… - Heliyon, 2023 - cell.com
The in vitro anticancer efficacy of a new series of quinazoline-based thiazole derivatives was
explored. Three cancer cell lines, MCF-7, HepG2, and A548, as well as the normal Vero cell …

Hybrid quinazoline 1, 3, 5‐triazines as epidermal growth factor receptor (EGFR) inhibitors with anticancer activity: design, synthesis, and computational study

P Pathak, H Rimac, M Grishina, A Verma… - …, 2021 - Wiley Online Library
We report a series of hybrid quinazoline‐1, 3, 5‐triazine derivatives as EGFR inhibitors,
which were synthesised and tested by using a variety of in vitro, in silico, and in vivo …

Synthesis and biological evaluation of novel [1, 2, 3] triazolo-pyrrolo [1, 2-a] pyrido [4, 3-d] pyrimidines as EGFR targeting anticancer agents

SR Bandi, N Kavitha, SK Nukala… - Journal of Molecular …, 2023 - Elsevier
Herein, we synthesized some new fused [1, 2, 3] triazolo-pyrrolo [1, 2-a] pyrido [4, 3-d]
pyrimidines via click chemistry followed by carbon-carbon bond coupling as key approach …

Design and Synthesis of some new 2, 4, 6-trisubstituted quinazoline EGFR inhibitors as targeted anticancer agents

HA Allam, EE Aly, AK Farouk, AM El Kerdawy… - Bioorganic …, 2020 - Elsevier
The present study describes the synthesis of 6-bromo-2-(pyridin-3-yl)-4-substituted
quinazolines starting from 4-chloro derivative VI via the reaction with either phenolic …

Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing oxazole or imidazole as potential EGFR inhibitors

Y OuYang, C Wang, B Zhao, H Xiong, Z Xiao… - New Journal of …, 2018 - pubs.rsc.org
Six series of quinazoline derivatives bearing oxazole or imidazole (8a–f, 9a–f, 10a–d, 11a–f,
12a–d and 13a–i) were designed, synthesized and their IC50 values evaluated against …

Imidazo [1, 2-a] quinazolines as novel, potent EGFR-TK inhibitors: Design, synthesis, bioactivity evaluation, and in silico studies

Z Hasanvand, TO Bakhshaiesh, F Peytam… - Bioorganic …, 2023 - Elsevier
Tyrosine protein kinases (TKs) have been proved to play substantial roles on many cellular
processes and their overexpression tend to be found in various types of cancers. Therefore …

Pharmacophore‐linked pyrazolo[3,4‐d]pyrimidines as EGFR‐TK inhibitors: Synthesis, anticancer evaluation, pharmacokinetics, and in silico mechanistic studies

AA Gaber, AM El‐Morsy, FF Sherbiny… - Archiv Der …, 2021 - Wiley Online Library
Targeting the epidermal growth factor receptors (EGFRs) with small inhibitor molecules has
been validated as a potential therapeutic strategy in cancer therapy. Pyrazolo [3, 4‐d] …