Tetrahedron letters

Synthesis of novel iodo derived bicalutamide analogs

VA Nair, SM Mustafa, ML Mohler, SJ Fisher, JT Dalton…

Index: Nair, Vipin A.; Mustafa, Suni M.; Mohler, Michael L.; Fisher, Scott J.; Dalton, James T.; Miller, Duane D. Tetrahedron Letters, 2004 , vol. 45, # 51 p. 9475 - 9477

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Citation Number: 25

Abstract

The search for nonsteroidal antiandrogens that will block the pharmacological effects of testosterone, led to the development of compounds like flutamide, nilutamide, and (R,S)-bicalutamide , which are widely used for the treatment of metastatic prostate cancer ( Scheme 1). [1], [2], [3] and [4] The commonly accepted structure–activity relationship borne out of these ligands suggest the importance of an electron deficient aromatic ring, branched alkyl group α to the amidic ...

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