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Letters in Organic Chemistry

Author(s): M. Sani, F. Viani, M. Binda, N. Zaffaroni and M. Zanda

DOI: 10.2174/1570178054405850

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Synthesis and in Vitro Anti-Proliferative Activity of Racemic Trifluoro-Casodex® (Bicalutamide)

Page: [447 - 449] Pages: 3

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Abstract

The trifluoro analogue 1 of Casodex® was synthesized in racemic form, according to a strategy based on the use of trifluoropyruvate as a key starting material. This compound showed significant in vitro antiproliferative activity on the human prostate cancer cell line LNCaP.

Keywords: prostate cancer, anti-androgen, trifluoro-casodex analogue, nucleophilic reagents, chromatography