1258161-07-7Relevant academic research and scientific papers
SAR based design of nicotinamides as a novel class of androgen receptor antagonists for prostate cancer
Yang, Su Hui,Song, Chin-Hee,Van, Hue Thi My,Park, Eunsook,Khadka, Daulat Bikram,Gong, Eun-Yeung,Lee, Keesook,Cho, Won-Jea
supporting information, p. 3414 - 3418 (2013/06/05)
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.
NEW NICOTINAMIDE DERIVATIVES WITH ANTI-ANDROGEN EFFECTS, PROCESSES OF PREPARING, AND ANTIANDROGENS COMPRISING THE SAME
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Page/Page column 15; 17; 18, (2010/12/29)
Provided are novel nicotinamide derivatives and pharmaceutically acceptable salts thereof with anti-androgen effects, preparing processes of the same and antiandrogens containing the same as active ingredients. More particularly, the said nicotinamide derivatives have anti-androgen activity, so that they can be effectively used as a preventive or therapeutic agent for androgen-related diseases such as prostatic disease, androgenic alopecia and acne.
