NOTICE: Due to a lapse in annual appropriations, most of this website is not being updated. Learn more.
Form submissions will still be accepted but will not receive responses at this time. Sections of this site for programs using non-appropriated funds (such as NVLAP) or those that are excepted from the shutdown (such as CHIPS and NVD) will continue to be updated.
An official website of the United States government
Here’s how you know
Official websites use .gov
A .gov website belongs to an official government organization in the United States.
Secure .gov websites use HTTPS
A lock (
) or https:// means you’ve safely connected to the .gov website. Share sensitive information only on official, secure websites.
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.
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 October 10, 2025)