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
em 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.
[Box see text].
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Ensaios de Seleção de Medicamentos Antitumorais
/
Desenho de Fármacos
/
Testes de Sensibilidade Microbiana
/
Escherichia coli
/
Antibacterianos
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Egito