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 and 4 ( [5-phenyl-2-[(4methylphenyl)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 (GI 50 ), 1.2-2.5 μM (TGI) and 5-6 μM (LC 50 ). It was found that the presence of phenyl or 4-methylphenyl groups at C(2) and C(5) in the oxazole ring is of critical importance for the manifestation of the anticancer activity. Matrix COMPARE analysis using LC 50 vector showed a high positive correlation of compound 9 with standard anticancer agents that can directly disrupt mitochondrial function, causing programmed death of cancer cells. The obtained results indicate the anticancer activity of 1,3-oxazol-4-ylphosphonium salts, which could be useful for developing new anticancer drugs. The most active of them can be recommended for further in-depth studies and synthesis of new derivatives with antitumor activity on their basis.

Design and Synthesis of Oxazole‐Linked Pyrazole Chalcone Derivatives: In‐Vitro Anticancer Evaluation and In‐Silico Molecular Docking Studies

“…[30][31][32] Oxazole nucleus attain much more attention due to its application in organic synthesis and their various pharmaceutical properties in various natural and unnatural structures. 1,3oxazole structures showed potent biological properties including insecticidal, [33] anti-tuberculosis, [34] herbicidal activity, [35] HIV-1 protease inhibitors, [36] and anticancer [37,38] activities.…”