In vitro and in silico evaluation of anticancer activity of new indole-based 1, 3, 4-oxadiazoles as EGFR and COX-2 inhibitors

B Sever, MD Altıntop, A Özdemir, G Akalın Çiftçi… - Molecules, 2020 - mdpi.com
Epidermal growth factor receptor (EGFR) and cyclooxygenase-2 (COX-2) are crucial
targetable enzymes in cancer management. Therefore, herein, new 2-[(5-((1 H-indol-3-yl) …

Development of pyridazine derivatives as potential EGFR inhibitors and apoptosis inducers: Design, synthesis, anticancer evaluation, and molecular modeling studies

MF Ahmed, EY Santali, EMM El-Deen, IA Naguib… - Bioorganic …, 2021 - Elsevier
Novel hybrids of pyridazine-pyrazoline were synthesized aiming to develop new
antiproliferative candidates. All compounds were submitted to the National Cancer Institute …

In silico screening of chalcone derivatives as promising EGFR-TK inhibitors for the clinical treatment of cancer

S Mathpal, T Joshi, P Sharma, P Maiti, M Nand… - 3 Biotech, 2024 - Springer
Epidermal growth factor receptor (EGFR) promotes tumorigenic characteristics and activates
cancer-associated signaling pathways such as Wnt/-catenin, transforming growth factor …

Design, synthesis and molecular modeling studies of 2-styrylquinazoline derivatives as EGFR inhibitors and apoptosis inducers

NH Amin, MT Elsaadi, SS Zaki, HM Abdel-Rahman - Bioorganic Chemistry, 2020 - Elsevier
Herein, we report the synthesis of novel 2-substituted styrylquinazolines conjugated with
aniline or sulfonamide moieties, anticipated to act as potent anticancer therapeutic agents …

Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents

J Ma, G Bao, L Wang, W Li, B Xu, B Du, J Lv… - European Journal of …, 2015 - Elsevier
Through a structure-based molecular hybridization approach, a series of novel
benzothiazole derivatives bearing indole-based moiety were designed, synthesized and …

Design, synthesis, in vitro, and in silico studies of new thiadiazol derivatives as promising VEGFR-2 inhibitors and apoptosis inducers

HA Mahdy, H Elkady, WE Elgammal… - Journal of Molecular …, 2024 - Elsevier
The presented study reports the synthesis, in silico and in vitro evaluations of a series of
novel thiadiazole derivatives designed with the pharmacophoric features of Vascular …

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 …

Synthesis, biological and computational evaluation of novel 2, 3-dihydro-2-aryl-4-(4-isobutylphenyl)-1, 5-benzothiazepine derivatives as anticancer and anti-EGFR …

AB Shaik, YR Prasad, S Nissankararao… - Anti-Cancer Agents …, 2020 - ingentaconnect.com
Background: Despite the availability of a variety of chemotherapeutic agents, cancer is still
one of the leading causes of death worldwide because of the problems with existing …

Design, synthesis, anti-proliferative evaluation, docking, and MD simulation studies of new thieno [2, 3-d] pyrimidines targeting VEGFR-2

SA El-Metwally, H Elkady, M Hagras, DZ Husein… - RSC …, 2023 - pubs.rsc.org
In this work, new thieno [2, 3-d] pyrimidine-derived compounds possessing potential
anticancer activities were designed and synthesized to target VEGFR-2. The thieno [2, 3-d] …

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 …