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

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

Document Type: Review Article

Affiliations: Dipartimento di Chimica, Materiali ed Ingegneria Chimica “G. Natta” del Politecnico di Milano and C.N.R .- Istituto di Chimica del Riconoscimento Molecolare, Sezione “A. Quilico”, via Mancinelli 7, I-20131 Milano, Italy.

Publication date: 01 August 2005

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  • Letters in Organic Chemistry publishes original letters on all areas of organic chemistry including synthesis, bioorganic, medicinal, natural products, organometallic, supramolecular, molecular recognition and physical organic chemistry. The emphasis is placed on publishing quality papers very rapidly. Letters are processed rapidly and take full advantage of the Internet technology both for the submission and the review of the manuscripts.
    The journal is essential reading for all organic chemists both in academia and industry.
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