Design and Synthesis of Non-Covalent Imidazo[1,2-a]quinoxaline-Based Inhibitors of EGFR and Their Anti-Cancer Assessment

M Kumar, G Joshi, S Arora, T Singh, S Biswas… - Molecules, 2021 - mdpi.com
A series of 30 non-covalent imidazo [1, 2-a] quinoxaline-based inhibitors of epidermal
growth factor receptor (EGFR) were designed and synthesized. EGFR inhibitory assessment …

Design, synthesis and anticervical cancer activity of new benzofuran–pyrazol-hydrazono-thiazolidin-4-one hybrids as potential EGFR inhibitors and apoptosis …

HAS Abbas, SS Abd El-Karim - Bioorganic chemistry, 2019 - Elsevier
This study represents the synthetic approaches of a new set of 2-(((3-(benzofuran-2-yl)-1-
phenyl-1H-pyrazol-4-yl) methylene) hydrazono)-5-(aryl) thiazolidin-4-one derivatives 4–22 …

Synthesis and evaluation of 2, 9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors

YY Hei, Y Shen, J Wang, H Zhang, HY Zhao… - Bioorganic & Medicinal …, 2018 - Elsevier
In present study, we described the synthesis and biological evaluation of a new class of
EGFR inhibitors containing 2, 9-disubstituted 8-phenylthio/phenylsulfinyl-9 H-purine …

Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity

YA Ammar, AMS El-Sharief, A Belal, SY Abbas… - European journal of …, 2018 - Elsevier
Abstract New series of 5-(morpholinosulfonyl) isatin derivatives were designed and
synthesized. The new compounds were characterized on the basis of spectral and …

Design, synthesis, and mechanistic insight of novel imidazolones as potential EGFR inhibitors and apoptosis inducers

FG Abdulrahman, HS Abulkhair, HS El Saeed… - Bioorganic …, 2024 - Elsevier
As regards to the structural analysis and optimization of diverse potential EGFR inhibitors,
two series of imidazolyl-2-cyanoprop-2-enimidothioates and ethyl …

Rational design and synthesis of novel quinazolinone N-acetohydrazides as type II multi-kinase inhibitors and potential anticancer agents

SS Abd El-Karim, YM Syam, AM El Kerdawy… - Bioorganic …, 2024 - Elsevier
In the current investigation, a new class of quinazolinone N-acetohydrazides 9a-v was
designed as type II multi-kinase inhibitors. The target quinazolinones were tailored so that …

Targeting EGFR tyrosine kinase: Synthesis, in vitro antitumor evaluation, and molecular modeling studies of benzothiazole-based derivatives

AM Mokhtar, SM El-Messery, MA Ghaly, GS Hassan - Bioorganic chemistry, 2020 - Elsevier
New benzothiazole-based derivatives were synthesized in the present work with the aim of
evaluating their antitumor activity. They were in vitro tested against hepatocellular carcinoma …

Synthesis and in vitro anticancer evaluation of some fused indazoles, quinazolines and quinolines as potential EGFR inhibitors

EA Abdelsalam, WA Zaghary, KM Amin… - Bioorganic …, 2019 - Elsevier
Abstract derivatives of benzo [g] indazole 5a, b, benzo [h] quinazoline 7, 12a-c, 13a-c and
15a-c and benzo [h] quinoline 17a-c and 19a-c were synthesized from 6-methoxy-3, 4 …

Design and evaluation of potent EGFR inhibitors through the incorporation of macrocyclic polyamine moieties into the 4-anilinoquinazoline scaffold

Y Ju, J Wu, X Yuan, L Zhao, G Zhang… - Journal of Medicinal …, 2018 - ACS Publications
Adenosine triphosphate (ATP)-competitive inhibitors of the epidermal growth factor receptor
(EGFR) have provided a significant improvement in the disease outcome of nonsmall cell …

Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines

RD Li, X Zhang, QY Li, ZM Ge, RT Li - Bioorganic & medicinal chemistry …, 2011 - Elsevier
On the basis of combination strategy, a novel series of EGFR inhibitors were designed and
synthesized by combination of dithiocarbamic acid esters and 4-anilinoquinazolines. The …