Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors

AM Srour, NS Ahmed, SS Abd El-Karim… - Bioorganic & Medicinal …, 2020 - Elsevier
Heterocyclic rings such as thiazole and benzimidazole are considered as privileged
structures, since they constitute several FDA-approved drugs for cancer treatment. In this …

Synthesis, anticancer activity and molecular modeling studies of 1, 2, 4-triazole derivatives as EGFR inhibitors

HAM El-Sherief, BGM Youssif, SNA Bukhari… - European journal of …, 2018 - Elsevier
A series of novel compounds carrying 1, 2, 4-triazole scaffold were prepared and evaluated
for their antiproliferative activities against NCI 60 cell line. Compounds 10 (a, c), 11 (ad), and …

Synthesis, antiproliferative, docking and DFT studies of benzimidazole derivatives as EGFR inhibitors

HA Alzahrani, MM Alam, AA Elhenawy… - Journal of Molecular …, 2022 - Elsevier
In the present work, new benzimidazole linked 1, 2, 3-triazole hybrids have been
synthesized and screened for antiproliferative and EGFR kinase inhibitory activities. The …

Novel 2-(5-Aryl-4, 5-dihydropyrazol-1-yl) thiazol-4-one as EGFR inhibitors: synthesis, biological assessment and molecular docking insights

T Al-Warhi, AM El Kerdawy, MA Said… - Drug Design …, 2023 - Taylor & Francis
Introduction Epidermal growth factor receptor (EGFR) regulates several cell functions which
include cell growth, survival, multiplication, differentiation, and apoptosis. Currently, EGFR …

New pyrimidine and pyrazole-based compounds as potential EGFR inhibitors: Synthesis, anticancer, antimicrobial evaluation and computational studies

IMM Othman, ZM Alamshany, NY Tashkandi… - Bioorganic …, 2021 - Elsevier
This study was focused on the synthesis of new pyrimidines 4a, b, 5a, b and pyrazoles 6a, b
as ATP mimicking tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR) …

New Thiazolyl-Pyrazoline derivatives as potential dual EGFR/HER2 inhibitors: design, synthesis, anticancer activity evaluation and in silico study

MM Fakhry, AA Mattar, M Alsulaimany, EM Al-Olayan… - Molecules, 2023 - mdpi.com
A new series of thiazolyl-pyrazoline derivatives (4a–d, 5a–d 6a, b, 7a–d, 8a, b, and 10a, b)
have been designed and synthesized through the combination of thiazole and pyrazoline …

Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors

KM Qiu, HH Wang, LM Wang, Y Luo, XH Yang… - Bioorganic & medicinal …, 2012 - Elsevier
A series of pyrazolyl-thiazolinone derivatives (E1–E36) have been designed and
synthesized and their biological activities were also evaluated as potential EGFR and HER …

Novel benzothiazole hybrids targeting EGFR: Design, synthesis, biological evaluation and molecular docking studies

EA Abd El-Meguid, GO Moustafa, HM Awad… - Journal of Molecular …, 2021 - Elsevier
Novel benzo [d] thiazole-based analogues were synthesized with the aim of screening their
in vitro anticancer activity. All the new derivatives 4–21 were evaluated against human …

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 and Biological Evaluation of Benzo [d] thiazolyl‐Sulfonyl‐Benzo [4, 5] isothiazolo [2, 3‐c][1, 2, 3] triazole Derivatives as EGFR Targeting Anticancer Agents

E Ramya Sucharitha, S Kumar Nukala… - …, 2023 - Wiley Online Library
A one‐step procedure for the synthesis of new fused Benzo [d] thiazolo‐1, 2, 3‐triazoles (3 a–
3 h and 4 a–4 h) in good yields using sulfonylazides (2) and iodoalkyne (1) through from the …