Design, synthesis and biological evaluation of novel pyrazole-based compounds as potential chemotherapeutic agents.
Future Med Chem
; 16(13): 1299-1311, 2024 Jul 02.
Article
en En
| MEDLINE
| ID: mdl-39109431
ABSTRACT
Aim:
Design and synthesis of pyrazole-based chemotherapeutic agents. Materials &methods:
A series of novel diphenyl pyrazole-chalcone derivatives were synthesized and assessed for their cytotoxic activities against 14 cancer cell lines and their antimicrobial activities against MRSA and Escherichia coli along with their safety using HSF normal cell line. Results &conclusion:
Majority of the compounds showed moderate-to-significant anticancer activity with selective high percentage inhibition (>80%) against HNO-97 while being nontoxic toward normal cells. Compounds 6b and 6d were the most potent congeners with IC50 of 10 and 10.56 µM respectively. The synthesized compounds exhibited moderate to potent antimicrobial activities. Interestingly, compound 6d exhibited a minimum inhibitory concentration of 15.7 µg/ml against MRSA; and a minimum inhibitory concentration of 7.8 µg/ml versus E. coli.
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Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirazoles
/
Ensayos de Selección de Medicamentos Antitumorales
/
Diseño de Fármacos
/
Pruebas de Sensibilidad Microbiana
/
Escherichia coli
/
Antibacterianos
/
Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
Future Med Chem
Año:
2024
Tipo del documento:
Article
País de afiliación:
Egipto