Thiazole-containing compounds have a wide range of anticancer activities. Dasatinib, a thiazole-containing compound, has been approved to treat leukemia. Ethisterone, a steroidal hormone, treats endometritis and mastalgia, inhibits gonadotrophins, and has androgenic effects. Fusion of steroid skeleton of ethisterone with thiazole yields potential anti-melanoma agents. Newly developed thiazolo-ethisterone derivatives have remarkable cytotoxicity against melanoma cell lines in vitro. Several of these compounds have shown potent activity against melanoma cell lines with 50% inhibitory concentration (IC50) as low as 1.77 μM. The most potent thiazolo-ethisterone derivative is more toxic than tamoxifen (chemotherapeutic treating breast cancer) in melanoma cell lines. Proteomics studies for the mode of action and in vivo antimelanoma properties of these potent compounds will be discussed in this presentation.

In vitro and in vivo anti-melanoma studies of thiazolo-ethisterone derivatives

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ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.