New quinazoline sulfonamide derivatives as potential anticancer agents: Identifying a promising hit with dual EGFR/VEGFR-2 inhibitory and radiosensitizing activity

MM Ghorab, AM Soliman, K El-Adl, NS Hanafy - Bioorganic Chemistry, 2023 - Elsevier
Herein, we report the synthesis of a series of new quinazoline sulfonamide conjugates 2–16
and their evaluation as potential anticancer agents via dual targeting of EGFR T790M and …

New thiazolidine-2, 4-diones as effective anti-proliferative and anti-VEGFR-2 agents: Design, synthesis, in vitro, docking, MD simulations, DFT, ADMET, and toxicity …

H Elkady, AA Abuelkhir, M Rashed, MS Taghour… - … Biology and Chemistry, 2023 - Elsevier
Abstract Novel thiazolidine-2, 4-dione derivatives, 11a-g, were designed, and synthesized
targeting the VEGFR-2 protein. The in vitro studies indicated the abilities of the synthesized …

Pyrazolo [3, 4-d] pyrimidine derivatives as EGFRT790M and VEGFR-2 dual TK inhibitors: Design, synthesis, molecular docking, ADMET profile and anticancer …

D Adel, K El-Adl, T Nasr, TM Sakr, W Zaghary - Journal of Molecular …, 2023 - Elsevier
Abstract Seventeen new pyrazolo [3, 4-d] pyrimidine derivatives have been designed,
created and tested as dual VEGFR-2 and EGFR inhibitors for their anticancer special effects …

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 …

Exploration of the VEGFR-2 inhibition activity of phthalazine derivatives: design, synthesis, cytotoxicity, ADMET, molecular docking and dynamic simulation

HH Bayoumi, MK Ibrahim, MA Dahab, F Khedr… - RSC …, 2024 - pubs.rsc.org
Novel phthalazine derivatives were designed, synthesized and evaluated against Hep G2
and MCF-7 as VEGFR-2 inhibitors. In particular, compounds 2g and 4a were found to be the …

Iodoquinazoline-derived VEGFR-2 and EGFRT790M dual inhibitors: Design, synthesis, molecular docking and anticancer evaluations

AA Mohamed, SSA El-Hddad, AKB Aljohani… - Bioorganic …, 2024 - Elsevier
Herein, we report the synthesis of a series of new fourteen iodoquinazoline derivatives 7a-c
to 13a-e and their evaluation as potential anticancer agents via dual targeting of EGFR …

Rationale, in silico docking, ADMET profile, design, synthesis and cytotoxicity evaluations of phthalazine derivatives as VEGFR-2 inhibitors and apoptosis inducers

HH Bayoumi, MK Ibrahim, MA Dahab, F Khedr… - RSC …, 2024 - pubs.rsc.org
New phthalazine derivatives as vascular endothelial growth factor receptor-2 (VEGFR-2)
inhibitors were synthesized joined to different spacers including pyrazole, α, β-unsaturated …

Design, synthesis, docking, ADMET and anticancer evaluations of N-alkyl substituted iodoquinazoline derivatives as dual VEGFR-2 and EGFR inhibitors

M Alsulaimany, K El-Adl, AKB Aljohani, HY Alharbi… - RSC …, 2023 - pubs.rsc.org
Fifteen new 1-alkyl-6-iodoquinazoline derivatives 5a–d to 9a–e were designed and
synthesized and their anticancer activities were evaluated against HepG2, MCF-7, HCT116 …

Exploration of cytotoxicity of iodoquinazoline derivatives as inhibitors of both VEGFR‐2 and EGFRT790M: Molecular docking, ADMET, design, and syntheses

M Alsulaimany, SSA El‐Hddad, ZSM Akrim… - Archiv der …, 2024 - Wiley Online Library
Novel inhibitors of epidermal growth factor receptor (EGFR) T790M/vascular endothelial
growth factor receptor‐2 (VEGFR‐2) were synthesized based on the iodoquinazoline …

Anticancer evaluations of iodoquinazoline substituted with allyl and/or benzyl as dual inhibitors of EGFR WT and EGFR T790M: design, synthesis, ADMET and …

AKB Aljohani, K El-Adl, B Almohaywi, OM Alatawi… - RSC …, 2024 - pubs.rsc.org
Fifteen new iodoquinazoline derivatives, 5a, b to 18, are reported in this study and their
anticancer evaluation as dual inhibitors of EGFRWT and EGFRT790M. The new derivatives …