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 …

Synthesis and biological evaluation of new derivatives of thieno-thiazole and dihydrothiazolo-thiazole scaffolds integrated with a pyrazoline nucleus as anticancer and …

IMM Othman, ZM Alamshany, NY Tashkandi… - RSC …, 2022 - pubs.rsc.org
Deregulation of various protein kinases is considered as one of the important factors
resulting in cancer development and metastasis, thus multi-targeting the kinase family is one …

Optimization and SAR investigation of novel 2, 3-dihydropyrazino [1, 2-a] indole-1, 4-dione derivatives as EGFR and BRAFV600E dual inhibitors with potent …

HAM Gomaa, ME Shaker, SI Alzarea, OM Hendawy… - Bioorganic …, 2022 - Elsevier
Using a single drug to treat cancer with dual-targeting is an unusual approach when
compared to other drug combinations. Dual-targeting agents were developed as a result of …

Rationale design and synthesis of new apoptotic thiadiazole derivatives targeting VEGFR-2: computational and in vitro studies

WE Elgammal, H Elkady, HA Mahdy, DZ Husein… - RSC …, 2023 - pubs.rsc.org
This work presents the synthesis and in vitro, and in silico analyses of new thiadiazole
derivatives that are designed to mimic the pharmacophoric characteristics of vascular …

Evaluation of the anti-proliferative activity of 2-oxo-pyridine and 1′ H-spiro-pyridine derivatives as a new class of EGFR Wt and VEGFR-2 inhibitors with apoptotic …

RR Raslan, YA Ammar, SA Fouad, SA Hessein… - RSC …, 2023 - pubs.rsc.org
Developing new agents for cancer treatment remains a top priority because it is one of the
deadliest worldwide. A new series of 2-oxo-pyridine and 1′ H-spiro-pyridine derivatives …

Novel quinoline-3-carboxamides (Part 2): Design, optimization and synthesis of quinoline based scaffold as EGFR inhibitors with potent anticancer activity

RM Aly, RAT Serya, AM El-Motwally, A Esmat… - Bioorganic …, 2017 - Elsevier
EGFR has a key role in cell growth. Its mutation and overexpression share in epithelial
malignancies and tumor growth. Quinazoline and quinoline derivatives are common …

Benzo [g] quinazolin-based scaffold derivatives as dual EGFR/HER2 inhibitors

MM Ghorab, MS Alsaid, AM Soliman… - Journal of Enzyme …, 2018 - Taylor & Francis
Targeting EGFR has proven to be beneficial in the treatment of several types of solid
tumours. So, a series of novel 2-(4-oxo-3-(4-sulfamoylphenyl)-3, 4-dihydrobenzo [g] …

Novel sulfonyl thiazolyl-hydrazone derivatives as EGFR inhibitors: Design, synthesis, biological evaluation and molecular docking studies

TA Farghaly, EMH Abbas, AM Al-Soliemy, R Sabour… - Bioorganic …, 2022 - Elsevier
New hydrazonoyl-sulfonylthiazoles were designed and synthesized as EGFR inhibitors. The
new sulfonylthiazole derivatives were assessed in vitro to measure their effect on EGFR …

New phthalimide-based derivatives as EGFR-TK inhibitors: Synthesis, biological evaluation, and molecular modeling study

NI Mansour, SM El-Sayed, NS El-Gohary… - Bioorganic …, 2022 - Elsevier
A novel series of phthalimide derivatives was synthesized and evaluated for in vitro
antitumor activity against six human cancer cell lines; HepG-2, HCT-116, MCF-7, Hep2, PC3 …

Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors

XX Tao, YT Duan, LW Chen, DJ Tang, MR Yang… - Bioorganic & Medicinal …, 2016 - Elsevier
A series of novel pyrazole-nitroimidazole derivatives had been arranged and evaluated for
their EGFR/HER-2 tyrosine kinase inhibitory activity as well as their antiproliferative …