Riham F George1. 1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
Abstract
AIM: Discovery of novel potent anticancer agents with lower side effects is a challenge to overcome cancer, the second leading cause of death. METHODOLOGY: 2-oxindole-based hydrazides (6a-g) and benzenesulfonyl hydrazides (9a-d) were synthesized by simple condensation reactions of the appropriate hydrazides (2a-g) or (8a-d) with 1-ethyl-2,3-oxindolinedione (4). They were screened for their cytotoxicity against HepG2 (liver), MCF-7 (breast), HCT116 (colon) and A549 (lung) cancer cell lines. RESULTS: The substituted benzohydrazides (6b-g) revealed higher activity and selectivity toward the tested cell lines than doxorubicin and 9a-d. Compound 6c exhibited the highest activity against MCF-7 cell line with IC50 = 0.0058 μM and it induced apoptosis by caspase-3 activation, Bax upregulation and Bcl-2 downregulation in a dose-dependent manner. CONCLUSION: This compound can be considered as a potent cytotoxic agent with apoptotic induction property.
AIM: Discovery of novel potent anticancer agents with lower side effects is a challenge to overcome cancer, the second leading cause of death. METHODOLOGY:2-oxindole-based hydrazides (6a-g) and benzenesulfonyl hydrazides (9a-d) were synthesized by simple condensation reactions of the appropriate hydrazides (2a-g) or (8a-d) with 1-ethyl-2,3-oxindolinedione (4). They were screened for their cytotoxicity against HepG2 (liver), MCF-7 (breast), HCT116 (colon) and A549 (lung) cancer cell lines. RESULTS: The substituted benzohydrazides (6b-g) revealed higher activity and selectivity toward the tested cell lines than doxorubicin and 9a-d. Compound 6c exhibited the highest activity against MCF-7 cell line with IC50 = 0.0058 μM and it induced apoptosis by caspase-3 activation, Bax upregulation and Bcl-2 downregulation in a dose-dependent manner. CONCLUSION: This compound can be considered as a potent cytotoxic agent with apoptotic induction property.
Authors: Alaa A-M Abdel-Aziz; Adel S El-Azab; Nawaf A AlSaif; Ahmad J Obaidullah; Abdulrahman M Al-Obaid; Ibrahim A Al-Suwaidan Journal: J Enzyme Inhib Med Chem Date: 2021-12 Impact factor: 5.051
Authors: Norhan H Mahdally; Riham F George; Mona T Kashef; Medhat Al-Ghobashy; Fathia E Murad; Ahmed S Attia Journal: Front Microbiol Date: 2021-07-05 Impact factor: 5.640