Hexafluoroisopropanol-Mediated Domino Reaction for the Synthesis of Thiazolo-androstenones: Potent Anticancer Agents

A cascade reaction
of thioamides with 6β-bromoandrostenedione
in hexafluoroisopropanol formed substituted thiazolo-androstenones.
This is a simple and mild protocol to synthesize novel molecules by
using readily available reagents and substrates. Feasibility of the
reaction has been rationalized by density functional theory calculations.
Moreover, these compounds are potent growth inhibitors of colon, central
nervous system, melanoma, ovarian, and renal cancer cell lines with
50% growth inhibition values as low as 1.04 μM.