5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells

27 novel 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A were designed and synthesized to make them more conducive to the cancer treatment. The antiproliferative activity of all the target compounds was tested against six human cancer cell lines and one human normal cell line. Compound 10d exhibited nearly the most potent cytotoxicity with IC50 values of 0.58, 0.69, 1.82, 0.85, 0.75, 0.33 and 1.75 & mu;M against A549, DU -145, A375, HeLa, HepG2, MDA-MB-231 and L-02 cell lines. Moreover, 10d inhibited metastasis and induced apoptosis of MDA-MB-231 cells in a dose-dependent manner. The potent anticancer effects of 10d were prompted based on the aforementioned results, the therapeutic potential of 10d for breast cancer was worth further exploration.

Automated summary

27 novel derivatives of 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione of brefeldin A were designed and synthesized for improved cancer treatment. The antiproliferative activity of all the compounds was tested against human cancer cell lines and a normal cell line. Compound 10d showed the most potent cytotoxicity, with significant inhibition of metastasis and induction of apoptosis in breast cancer cells.