Abstract
A series of new 2-aryl 5-sulfonyl-1,3-oxazole-4-carboxylates for NCI anticancer screening protocol against 60 cancer cell lines were synthesized. Screening was performed in vitro on 60 cell lines of lungs, kidneys, CNS, ovaries, prostate, and breast cancer, leukemia, and melanoma. Methyl 5-benzylsulfonyl-2-phenyl-1,3-oxazole-4-carboxylate 15 exhibited potent and broad range of cytotoxic activity against tested human cancer cells with average GI50, TGI, and LC50 values of 5.37·10-6, 1.29·10-5 and 3.6·10-5 mol/L respectively. Molecular docking was used to evaluate the possible interaction of compound 15 with tubulin as well as a complex formation with CDK2.
Highlights
During the last years, the search for new biologically active compounds, in particular anticancer agents, among 1,3-oxazole-4-carboxylates has stimulated considerable synthetic efforts [1,2,3]
It has been proposed that possible ways of anticancer influence of sulfonamide derivatives are associated with inhibition of the tubulin polymerization, similar to E7010 [5], DNA damage, BCL6, and NSD2 inhibition [6]
The synthesis of target compounds was accomplished by the reaction sequence illustrated in Scheme 1 and 2
Summary
The search for new biologically active compounds, in particular anticancer agents, among 1,3-oxazole-4-carboxylates has stimulated considerable synthetic efforts [1,2,3]. The synthesized 5-sulfonyl-1,3-oxazole-4-carboxylates were screened on human cancer cell lines at the NIH, Bethesda, Maryland, USA, under the drug discovery program of the NCI. The most active methyl 5-(benzylsulfonyl)2-phenyl-1,3-oxazole-4-carboxylate (15) had anticancer activity range from -78.70 to 109.63%.
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