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Molecules ; 28(3)2023 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-36770674

RESUMO

Acetylated triterpenoids betulin, oleanolic acid, ursolic acid, and glycyrrhetinic acid were converted into their succinyl-spacered acetazolamide conjugates. These conjugates were screened for their inhibitory activity onto carbonic anhydrase II and their cytotoxicity employing several human tumor cell lines and non-malignant fibroblasts. As a result, the best inhibitors were derived from betulin and glycyrrhetinic acid while those derived from ursolic or oleanolic acid were significantly weaker inhibitors but also of diminished cytotoxicity. A betulin-derived conjugate held a Ki = 0.129 µM and an EC50 = 8.5 µM for human A375 melanoma cells.


Assuntos
Ácido Glicirretínico , Ácido Oleanólico , Triterpenos , Humanos , Acetazolamida/farmacologia , Acetazolamida/química , Estrutura Molecular , Relação Estrutura-Atividade , Triterpenos/farmacologia , Triterpenos/química , Anidrase Carbônica II , Linhagem Celular Tumoral , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Anidrase Carbônica/química
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