New series of VEGFR-2 inhibitors and apoptosis enhancers: Design, synthesis and biological evaluation

AE Abdallah, RR Mabrouk, MR Elnagar… - Drug Design …, 2023 - Taylor & Francis
Background Cancer is still a major world health threat, causing a high rate of mortality.
VEGFR-2 inhibitor anticancer agents are of great significance. However, they showed some …

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 …

New proapoptotic chemotherapeutic agents based on the quinolone-3-carboxamide scaffold acting by VEGFR-2 inhibition

ZS El-Fakharany, YM Nissan, NK Sedky, RK Arafa… - Scientific Reports, 2023 - nature.com
In the current study, we designed and synthesized a series of new quinoline derivatives 10a-
p as antiproliferative agents targeting cancer through inhibition of VEGFR-2. Preliminary …

Discovery of novel VEGFR-2 inhibitors. Part II: Biphenyl urea incorporated with salicylaldoxime

H Gao, P Su, Y Shi, X Shen, Y Zhang, J Dong… - European Journal of …, 2015 - Elsevier
A series of novel VEGFR-2 inhibitors containing oxime as hinge binding fragment were
described. A strategy of pseudo six-membered ring formed through intramolecular hydrogen …

[HTML][HTML] Synthesis, anticancer, apoptosis-inducing activities and EGFR and VEGFR2 assay mechanistic studies of 5, 5-diphenylimidazolidine-2, 4-dione derivatives …

HM Alkahtani, MM Alanazi, FS Aleanizy… - Saudi Pharmaceutical …, 2019 - Elsevier
Abstract A new series of 5, 5-diphenylhydantoin derivatives containing benzylidene or isatin
(4–19) was synthesized. Their anticancer activity against HeLa, a cervical cancer cell line …

Design, synthesis, docking, DFT, MD simulation studies of a new nicotinamide-based derivative: In vitro anticancer and VEGFR-2 inhibitory effects

EB Elkaeed, RG Yousef, H Elkady, IMM Gobaara… - Molecules, 2022 - mdpi.com
A nicotinamide-based derivative was designed as an antiproliferative VEGFR-2 inhibitor
with the key pharmacophoric features needed to interact with the VEGFR-2 catalytic pocket …

Design, synthesis and biological evaluation of quinoline amide derivatives as novel VEGFR-2 inhibitors

Y Yang, L Shi, Y Zhou, HQ Li, ZW Zhu… - Bioorganic & medicinal …, 2010 - Elsevier
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in the process
of cancer angiogenesis. A series of quinoline amide derivatives were prepared and found to …

New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies

EB Elkaeed, MS Taghour, HA Mahdy… - Journal of Enzyme …, 2022 - Taylor & Francis
New quinoline and isatin derivatives having the main characteristics of VEGFR-2 inhibitors
was synthesised. The antiproliferative effects of these compounds were estimated against …

3D-QSAR pharmacophore modelling, virtual screening and docking studies for lead discovery of a novel scaffold for VEGFR 2 inhibitors: design, synthesis and …

MK Sobhy, S Mowafy, DS Lasheen, NA Farag… - Bioorganic …, 2019 - Elsevier
Abstract A series of novel 6, 7-dihydro-5H-cyclopenta [d] pyrimidine derivatives was
successfully designed, synthesized and evaluated as a new chemical scaffold with vascular …

New theobromine derivatives inhibiting VEGFR-2: design, synthesis, antiproliferative, docking and molecular dynamics simulations

HA Mahdy, H Elkady, MS Taghour, A Elwan… - Future Medicinal …, 2023 - Future Science
Background: VEGFR-2 is one of the most effective targets in cancer treatment. Aim: The
design and semi-synthesis of new theobromine derivatives as potential VEGFR-2 inhibitors …