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Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors

Published

Author(s)

Edward Sisco, Korry Barnes

Abstract

A series of novel 1,3-oxazole sulfonamides were constructed and screened for their potential to inhibit cancer cell growth. These compounds were evaluated against the full NCI-60 human tumor cell lines; with the majority exhibiting promising overall growth inhibitory properties. They displayed high specificity within the panel of leukemia cell lines vs. all other lines tested. When examined in the dose-response assay GI50 values fell within the low micromolar to nanomolar ranges. 1,3-oxazole sulfonamide 16 displayed the best average growth inhibition, while the 2-chloro-5-methyl (44) and 1-naphthyl (58) analogues proved to be the most potent leukemia inhibitors with mean GI50 values of 48.8 and 44.7 nanomolar respective-ly. In vitro tubulin polymerization experiments revealed that this class of compounds effectively binds to tubulin and induc-es depolymerization of microtubules within cells.
Citation
ACS Medicinal Chemical Letters
Volume
12
Issue
6

Keywords

Small molecules, anticancer drug leads, sulfonamides, heterocycles, oxazoles

Citation

Sisco, E. and Barnes, K. (2021), Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors, ACS Medicinal Chemical Letters, [online], https://doi.org/10.1021/acsmedchemlett.1c00219, https://tsapps.nist.gov/publication/get_pdf.cfm?pub_id=932076 (Accessed July 27, 2021)
Created June 17, 2021