Gallic acid based steroidal phenstatin analogues for selective targeting of breast cancer cells through inhibiting tubulin polymerization

Phenstatin analogues were synthesized on steroidal framework, for selective targeting of breast cancer cells. These analogues were evaluated for anticancer efficacy against breast cancer cell lines. Analogues 12 and 19 exhibited significant anticancer activity against MCF-7, hormone dependent breast cancer cell line. While analogues 10–14 exhibited significant anticancer activity against MDA-MB-231, hormone independent breast cancer cell line. Compound 10 showed significant oestrogen antagonistic activities with low agonistic activity in in vivo rat model. These analogues also retain tubulin polymerization inhibition activity. The most active analogue 10 was found to be non-toxic in Swiss albino mice up to 300 mg/kg dose. Gallic acid based phenstatin analogues may further be optimized as selective anti-breast cancer agents.

Phenstatin analogues on steroidal framework have been synthesized. Analogue 10 exhibited potent tubulin polymerization inhibition activity and was found to be non-toxic in Swiss albino mice.Figure optionsDownload as PowerPoint slideHighlights
► Steroidal phenstatin analogues exhibited selective antibreast cancer activity.
► Compound 10, cytotoxicity (IC50 = 5 μM) and antitubulin activity (IC50 = 0.99 μM).
► Compound 10, in vivo toxicity – safe up to 300 mg/kg dose.