Novel scaffold hopping of potent benzothiazole and isatin analogues linked to 1, 2, 3-triazole fragment that mimic quinazoline epidermal growth factor receptor …

N Rezki, MA Almehmadi, S Ihmaid, AM Shehata… - Bioorganic …, 2020 - Elsevier
A series of benzothiazole/isatin linked to 1, 2, 3-triazole moiety and terminal sulpha drugs 5a-
e and 6a-e were synthesized and evaluated for cytotoxic activity against a panel of cancer …

[HTML][HTML] 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 …

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, 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 …

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 …

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

PC Lv, CF Zhou, J Chen, PG Liu, KR Wang… - Bioorganic & medicinal …, 2010 - Elsevier
Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase
inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 …

Design, synthesis, molecular docking and antiproliferative activity of some novel benzothiazole derivatives targeting EGFR/HER2 and TS

KRA Abdellatif, A Belal, MT El-Saadi, NH Amin… - Bioorganic …, 2020 - Elsevier
Multi-targeted anticancer drugs are in focus as a promising research topic. A new series of
benzothiazoles hybridized with pyrimidine moiety was designed and synthesized using 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 …

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 …

Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents

PC Lv, HQ Li, J Sun, Y Zhou, HL Zhu - Bioorganic & medicinal chemistry, 2010 - Elsevier
Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been
discovered. Some of them exhibited significant EGFR inhibitory activity. Compound 3-(3, 4 …