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 …

Design, synthesis, in silico studies, and biological evaluation of novel pyrimidine-5-carbonitrile derivatives as potential anti-proliferative agents, VEGFR-2 inhibitors …

AM Saleh, HA Mahdy, MA El-Zahabi, ABM Mehany… - RSC …, 2023 - pubs.rsc.org
A novel series of pyrimidine-5-carbonitrile derivatives bearing benzylidene and hydrazone
moieties with different linkers (spacers) were designed and synthesized as possible …

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 …

Novel hydrazone‐isatin derivatives as potential EGFR inhibitors: Synthesis and in vitro pharmacological profiling

MF Ahmed, R El‐Haggar, AH Almalki… - Archiv der …, 2023 - Wiley Online Library
Merging isatin and arylhydrazone moieties constitutes an efficient strategy to access new
potential anticancer derivatives. Consequently, 14 hydrazone‐isatin derivatives were …

Targeting disease with benzoxazoles: a comprehensive review of recent developments

A Abdullahi, KY Yeong - Medicinal Chemistry Research, 2024 - Springer
Benzoxazole is an attractive scaffold in medicinal chemistry due to its diverse biological
applications. From 2016 to 2023, a plethora of benzoxazole derivatives have been …

Novel N-Arylmethyl-aniline/chalcone hybrids as potential VEGFR inhibitors: synthesis, biological evaluations, and molecular dynamic simulations

H Haffez, NA Elsayed, MF Ahmed… - Journal of Enzyme …, 2023 - Taylor & Francis
Significant advancements have been made in the domain of targeted anticancer therapy for
the management of malignancies in recent times. VEGFR-2 is characterised by its pivotal …

New thiazolidine-2, 4-diones as potential anticancer agents and apoptotic inducers targeting VEGFR-2 kinase: Design, synthesis, in silico and in vitro studies

H Elkady, HA Mahdy, MS Taghour, MA Dahab… - … et Biophysica Acta (BBA …, 2024 - Elsevier
Background VEGFR-2 has emerged as a prominent positive regulator of cancer
progression. Aim Discovery of new anticancer agents and apoptotic inducers targeting …

3-Substituted-2, 3-dihydrothiazole as a promising scaffold to design EGFR inhibitors

R El-Haggar, SF Hammad, RI Alsantali, MM Alrooqi… - Bioorganic …, 2022 - Elsevier
The overexpression of EGFR has been recognized as the driver mechanism in the
development of several human malignancies and the clinical use of EGFR inhibitors …

Benzoxazole or Benzothiazole as an Innate Directing Group for Palladium-and Ruthenium-Catalyzed Complementary C–H Arylation: Functionalization of Biorelevant …

M Maingle, S Sunny, L Sheeba, FR Pathan, K Seth - Synthesis, 2024 - thieme-connect.com
The benzoxazole and benzothiazole moieties were used as innate directing groups for Pd
(II)-and Ru (II)-catalyzed C–H arylation of the biorelevant heterocycles 2-arylbenzoxazole …

In silico insights into design of novel VEGFR-2 inhibitors: SMILES-based QSAR modelling, and docking studies on substituted benzo-fused heteronuclear derivatives

S Gupta, M Kashyap, Y Bansal… - SAR and QSAR in …, 2024 - Taylor & Francis
ABSTRACT Eight QSAR models (M1–M8) were developed from a dataset of 118 benzo-
fused heteronuclear derivatives targeting VEGFR-2 by Monte Carlo optimization method of …