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Evaluation of Anticancer Activity of 1,3-Oxazol-4-ylphosphonium Salts in Vitro.


ABSTRACT: A novel series of 1,3-oxazol-4-yltriphenylphosphonium salts has been synthesized and functionalized. Oxazole derivatives were subjected to NCI in vitro assessment. Seven most active derivatives have been selected for five-dose assay. Among them, compounds 9 ([2-(4-methylphenyl)-5-[(4-methylphenyl)sulfanyl]-1,3-oxazol-4-yl]triphenylphosphonium perchlorate), 1 ([5-(4-methylphenyl)amino]-2-phenyl-1,3-oxazol-4-yl]triphenylphosphonium perchlorate) and 4 ([5-phenyl-2-[(4-methylphenyl)amino]-1,3-oxazol-4-yl]triphenylphosphonium perchlorate) were the most active against all tested cancer subpanels. Statistical analysis of the total panel data showed average values of parameters of anticancer activity in the range of 0.3-1.1 μM (GI50 ), 1.2-2.5 μM (TGI) and 5-6 μM (LC50 ). It

SUBMITTER: Brusnakov M 

PROVIDER: S-EPMC9825890 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature