Caspase‐3: A primary target for natural and synthetic compounds for cancer therapy

P Yadav, R Yadav, S Jain… - Chemical biology & drug …, 2021 - Wiley Online Library
Caspases, a group of protease enzymes (cysteine proteases), exist as inactive zymogens in
the cells and execute apoptosis (programmed cell death). Caspase‐3, an executioner …

Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro …

AA Al-Karmalawy, MS Nafie, MA Shaldam… - Journal of Medicinal …, 2022 - ACS Publications
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 is a non-
nucleoside selective telomerase inhibitor; however, it experiences ineligible …

Caspase-3 activators as anticancer agents

N Srivastava, AK Saxena - Current Protein and Peptide Science, 2023 - ingentaconnect.com
Background: The cancer is still a major cause of death worldwide. Among different targets to
design anticancer agents, caspase-3 is an important target as its cleavage and activation …

Discovery of new pyrimidine-5-carbonitrile derivatives as anticancer agents targeting EGFR WT and EGFR T790M

AA Nasser, IH Eissa, MR Oun, MA El-Zahabi… - Organic & …, 2020 - pubs.rsc.org
A new series of pyrimidine-5-carbonitrile derivatives has been designed as ATP mimicking
tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR). These compounds …

New quinoxaline-based VEGFR-2 inhibitors: Design, synthesis, and antiproliferative evaluation with in silico docking, ADMET, toxicity, and DFT studies

MM Alanazi, H Elkady, NA Alsaif, AJ Obaidullah… - RSC …, 2021 - pubs.rsc.org
A new series of 3-methylquinoxaline-based derivatives having the same essential
pharmacophoric features as VEGFR-2 inhibitors have been synthesized and evaluated for …

New quinoxaline derivatives as VEGFR-2 inhibitors with anticancer and apoptotic activity: Design, molecular modeling, and synthesis

NA Alsaif, MA Dahab, MM Alanazi, AJ Obaidullah… - Bioorganic …, 2021 - Elsevier
Abstract New series of [1, 2, 4] triazolo [4, 3-a] quinoxalin-4 (5H)-one and [1, 2, 4] triazolo [4,
3-a] quinoxaline derivatives have been designed, synthesized, and biologically assessed for …

New bis ([1, 2, 4] triazolo)[4, 3-a: 3′, 4′-c] quinoxaline derivatives as VEGFR-2 inhibitors and apoptosis inducers: Design, synthesis, in silico studies, and anticancer …

MM Alanazi, HA Mahdy, NA Alsaif, AJ Obaidullah… - Bioorganic …, 2021 - Elsevier
A new series of bis ([1, 2, 4] triazolo)[4, 3-a: 3′, 4′-c] quinoxaline derivatives were
designed and synthesized to have the main essential pharmacophoric features of VEGFR-2 …

Design, synthesis, and biological evaluation of new challenging thalidomide analogs as potential anticancer immunomodulatory agents

MA El-Zahabi, H Sakr, K El-Adl, M Zayed… - Bioorganic …, 2020 - Elsevier
Thalidomide and its analogs are immunomodulatory drugs that inhibit the production of
certain inflammatory mediators associated with cancer. In the present work, a new series of …

Design, molecular docking, in vitro, and in vivo studies of new quinazolin-4 (3H)-ones as VEGFR-2 inhibitors with potential activity against hepatocellular carcinoma

IH Eissa, MK Ibrahim, AM Metwaly, A Belal… - Bioorganic …, 2021 - Elsevier
A series of new VEGFR-2 inhibitors were designed, synthesized and evaluated for their anti-
proliferative activities against hepatocellular carcinoma (HepG-2 cell line). Compound 29 b …

Development of isatin-thiazolo [3, 2-a] benzimidazole hybrids as novel CDK2 inhibitors with potent in vitro apoptotic anti-proliferative activity: Synthesis, biological and …

WM Eldehna, MA El Hassab, MF Abo-Ashour… - Bioorganic …, 2021 - Elsevier
In the current medical era, human health is experiencing numerous challenges, particularly
the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be …