Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis, biological …

SM Al-Muntaser, AA Al-Karmalawy, AM El-Naggar… - RSC …, 2023 - pubs.rsc.org
In this article, we continued our previous effort to develop new selective anticancer
candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 …

Design, synthesis, and SAR studies of novel 4-methoxyphenyl pyrazole and pyrimidine derivatives as potential dual tyrosine kinase inhibitors targeting both EGFR …

AM El-Naggar, AMA Hassan, EB Elkaeed… - Bioorganic …, 2022 - Elsevier
Guided by the pharmacophoric features of both EGFR and VEGFR-2 antagonists, two novel
series of 4-methoxyphenyl pyrazole and pyrimidine derivatives [(4a-c) and (5a-c, 6, 7a-c, 8 …

Design, synthesis, in vitro biological assessment and molecular modeling insights for novel 3-(naphthalen-1-yl)-4, 5-dihydropyrazoles as anticancer agents with …

WM Eldehna, MA El Hassab, ZM Elsayed, T Al-Warhi… - Scientific reports, 2022 - nature.com
Currently, the humanity is in a fierce battle against various health-related challenges
especially those associated with human malignancies. This created the urge to develop …

EGFR/VEGFR-2 dual inhibitor and apoptotic inducer: Design, synthesis, anticancer activity and docking study of new 2-thioxoimidazolidin-4one derivatives

AAE Mourad, NA Farouk, ESH El-Sayed, ARE Mahdy - Life Sciences, 2021 - Elsevier
Aims EGFR and VEGFR-2 have emerged as promising targets for cancer management as
they play a crucial role in tumor growth, angiogenesis and metastasis. A novel series of 2 …

Design, synthesis, in silico docking, ADMET and anticancer evaluations of thiazolidine-2, 4-diones bearing heterocyclic rings as dual VEGFR-2/EGFR T790M tyrosine …

NAAM Aziz, RF George, K El-Adl, WR Mahmoud - RSC advances, 2022 - pubs.rsc.org
Fourteen recent thiazolidine-2, 4-diones bearing furan and/or thiophene heterocyclic rings
have been designed, synthesized and assessed for their anticancer activities against four …

Design and synthesis of new thiazolidinone/uracil derivatives as antiproliferative agents targeting EGFR and/or BRAFV600E

MB Alshammari, AA Aly, BGM Youssif, S Bräse… - Frontiers in …, 2022 - frontiersin.org
Thiourea derivatives of uracil were efficiently synthesized via the reaction of 5-aminouracil
with isothiocyanates. Then, we prepared uracil-containing thiazoles via condensation of …

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) …

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 …

Five and six membered heterocyclic rings endowed with azobenzene as dual EGFR T790M and VEGFR-2 inhibitors: design, synthesis, in silico ADMET profile …

KE Anwer, SSA El-Hddad, NEA Abd El-Sattar… - RSC …, 2023 - pubs.rsc.org
Novel azobenzene scaffold-joined heterocyclic isoxazole, pyrazole, triazole, and/or triazine
moieties have been developed and synthesized utilizing microwave and traditional …

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 …