Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRWT, EGFRT790M, and EGFRL858R)

MG Abo Al-Hamd, HO Tawfik, O Abdullah… - Journal of Enzyme …, 2023 - Taylor & Francis
Hexahydroquinoline (HHQ) scaffold was constructed and recruited for development of new
series of anticancer agents. Thirty-two new compounds were synthesised where x-ray …

Exploring the interaction between epidermal growth factor receptor tyrosine kinase and some of the synthesized inhibitors using combination of in-silico and in-vitro …

RR Nasab, M Mansourian… - Research in …, 2018 - journals.lww.com
Quinazoline derivatives are potent inhibitors of human epidermal growth factor receptor
(EGFR) as anticancer agents. In this study, the cytotoxic effects of a new series of …

Synthesis of Quinoline‐Thiazolidine‐2, 4‐dione Coupled Pyrazoles as in vitro EGFR Targeting Anti‐Breast Cancer Agents and Their in silico Studies

M Bangaru, S Kumar Nukala, PK Kannekanti… - …, 2023 - Wiley Online Library
The synthesis of some new quinoline‐thiazolidine‐2, 4‐dione coupled pyrazoles (7 a–7 n)
via Knoevengal condensation, N‐alkynylation and tandem one‐pot Sonogashira coupling …

Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors

X Qin, Y Lv, P Liu, Z Li, L Hu, C Zeng, L Yang - Bioorganic & medicinal …, 2016 - Elsevier
A series of novel morpholin-3-one-fused quinazoline derivatives were designed,
synthesized and evaluated as EGFR tyrosine kinase inhibitors. Nineteen compounds …

Discovery of new pyrimido [5, 4-c] quinolines as potential antiproliferative agents with multitarget actions: Rapid synthesis, docking, and ADME studies

RA Mekheimer, SMR Allam, MA Al-Sheikh… - Bioorganic …, 2022 - Elsevier
A novel series of pyrimido [5, 4-c] quinoline derivatives variously substituted at positions 2
and 5 have been synthesized, in good to excellent yields, via rapid base-catalyzed …

Design, synthesis, anticancer evaluation, and in silico studies of some thieno[2,3‐d]pyrimidine derivatives as EGFR inhibitors

MTM Sayed, PA Halim, AK El‐Ansary… - Drug Development …, 2023 - Wiley Online Library
Abstract New series of 20 thieno [2, 3‐d] pyrimidine derivatives have been synthesized. The
National Cancer Institute evaluated all the newly synthesized compounds for their …

Synthesis, characterization, screening and docking analysis of 4-anilinoquinazoline derivatives as tyrosine kinase inhibitors

S Lü, W Zheng, L Ji, Q Luo, X Hao, X Li… - European Journal of …, 2013 - Elsevier
We report here the design and synthesis of a series of 4-anilinoquinazoline derivatives, of
which 7 compounds were crystallographically characterized, as epidermal growth factor …

Structure-based virtual screening, molecular docking, molecular dynamics simulation, and metabolic reactivity studies of quinazoline derivatives for their anti-EGFR …

AA Shah, S Ahmad, MK Yadav, K Raza… - Current Medicinal …, 2024 - ingentaconnect.com
Background: Epidermal growth factor receptor (EGFR/HER-1) and its role in tumor
development and progression through the mechanism of tumor angiogenesis is prevalent in …

In silico design, synthesis and activity of potential drug-like chrysin scaffold-derived selective EGFR inhibitors as anticancer agents

S Debnath, M Kanakaraju, M Islam, R Yeeravalli… - … biology and chemistry, 2019 - Elsevier
Background & objective Epidermal growth factor receptor (EGFR) signaling pathway is one
of the promising and well-established targets for anticancer therapy. The objective of the …

In vitro cytotoxicity and docking study of novel symmetric and asymmetric dihydropyridines and pyridines as EGFR tyrosine kinase inhibitors

B Mansour, WA Bayoumi, MA El‐Sayed… - Chemical biology & …, 2022 - Wiley Online Library
Quinolines have a weighty effect as anticancer agents and 1, 4‐DHPs have demonstrated
efficacy as anticancer agents in several studies, as well. New hybrid models of symmetric …