Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer

EA Abdelsalam, AA Abd El-Hafeez… - Journal of enzyme …, 2022 - Taylor & Francis
New series of thiazolyl-pyrazoline derivatives (7a–7d, 10a–10d and 13a–13f) have been
synthesised and assessed for their potential EGFR and VEGFR-2 inhibitory activities …

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 …

[HTML][HTML] Novel anticancer fused pyrazole derivatives as EGFR and VEGFR-2 dual TK inhibitors

NM Saleh, MG El-Gazzar, HM Aly, RA Othman - Frontiers in chemistry, 2020 - frontiersin.org
EGFR and VEGFR-2 represent promising targets for cancer treatment as they are very
important in tumor development as well as in angiogenesis and metastasis. In this work, 6 …

Novel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profile

AES Mghwary, EM Gedawy, AM Kamal… - Journal of enzyme …, 2019 - Taylor & Francis
Aim: Design and synthesis of thienopyrimidine derivatives as dual EGFR and VEGFR-2
inhibitors. Material and methods: A series of novel 6, 7, 8, 9-tetrahydro-5 H-cyclohepta [4, 5] …

Synthesis and anti-proliferative activity of some new quinoline based 4, 5-dihydropyrazoles and their thiazole hybrids as EGFR inhibitors

RF George, EM Samir, MN Abdelhamed… - Bioorganic …, 2019 - Elsevier
Abstract Quinoline derivatives 2, 3, quinolinyl based pyrazolines 4a, b, 5 and quinolinyl
pyrazolinyl thiazole hybrids 6a-d, 7a-c and 8a-d were synthesized and screened for their …

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 …

Novel benzothiazole-based dual VEGFR-2/EGFR inhibitors targeting breast and liver cancers: Synthesis, cytotoxic activity, QSAR and molecular docking studies

EA Abd El-Meguid, AM Naglah, GO Moustafa… - Bioorganic & Medicinal …, 2022 - Elsevier
A novel series of benzothiazole-based derivatives linked to various amino acids and their
corresponding ethyl ester analogues were prepared and were initially evaluated for their …

New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study

MM Al-Sanea, A Hamdi, AAB Mohamed… - Journal of enzyme …, 2023 - Taylor & Francis
A new series of 2-aminobenzothiazole hybrids linked to thiazolidine-2, 4-dione 4a–e, 1, 3, 4-
thiadiazole aryl urea 6a–d, and cyanothiouracil moieties 8a–d was synthesised. The in vitro …

[HTML][HTML] Synthesis, biological evaluation and computer-aided discovery of new thiazolidine-2, 4-dione derivatives as potential antitumor VEGFR-2 inhibitors

H Elkady, OA El-Dardir, A Elwan, MS Taghour… - RSC …, 2023 - pubs.rsc.org
In this study, novel VEGFR-2-targeting thiazolidine-2, 4-dione derivatives with potential
anticancer properties were designed and synthesized. The ability of the designed …

Discovery of new quinazolin-4 (3H)-ones as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative evaluation

IH Eissa, AGA El-Helby, HA Mahdy, MM Khalifa… - Bioorganic …, 2020 - Elsevier
Sixteen novel quinazoline-based derivatives were designed and synthesized via
modification of the VEGFR-2 reported inhibitor 7 in order to increase the binding affinity of …