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J Med Chem. 2013 Apr 25;56(8):3414-8. doi: 10.1021/jm3014103. Epub 2013 Apr 5.

SAR based design of nicotinamides as a novel class of androgen receptor antagonists for prostate cancer.

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College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwang-ju 500-757, Republic of Korea.


Molecular knowledge of pure antagonism and systematic SAR study offered a direction for structural optimization of DIMN to provide nicotinamides as a novel series of AR antagonists. Nicotinamides with extended linear scaffold bearing sterically bulky alkoxy groups on isoquinoline end were synthesized for H12 displacement. AR binding affinity and molecular basis of antiandrogenic effect establish the optimized derivatives, 7au and 7bb, as promising candidates of second generation AR antagonists for advanced prostate cancer.

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