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Biochem Biophys Res Commun. 2011 Jan 7;404(1):40-5. doi: 10.1016/j.bbrc.2010.11.049. Epub 2010 Nov 19.

Centchroman inhibits proliferation of head and neck cancer cells through the modulation of PI3K/mTOR pathway.

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Department of Radiotherapy, C.S.M. Medical University, Lucknow, Uttar Pradesh 226003, India.


Centchroman (CC; 67/20; INN: Ormeloxifene) is a non-steroidal antiestrogen extensively used as a female contraceptive in India. In the present study, we report the anti-proliferative effect of CC in head and neck squamous cell carcinoma (HNSCC) cells. CC inhibited cell proliferation in a dose dependent manner at 24 h of treatment. Further studies showed that CC treatment induced apoptosis, inhibited Akt/mTOR and signal transducers and activators of transcription protein 3 (STAT3) signaling, altered proteins associated with cell cycle regulation and DNA damage and inhibited colony forming efficiency of HNSCC cells. In addition, CC displayed anti-proliferative activity against a variety of non-HNSCC cell lines of diverse origin. The ability of CC to serve as a dual-inhibitor of Akt/mTOR and STAT3 signaling warrants further studies into its role as a therapeutic strategy against HNSCC.

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