Metabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer was written by Yu, Jiang;Zhou, Peiting;Du, Wu;Xu, Ruixue;Yan, Guoyi;Deng, Yufang;Li, Xinghai;Chen, Yuanwei. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020.Application In Synthesis of 2-Chloro-4-iodobenzonitrile The following contents are mentioned in the article:
Androgen receptor (AR) is a crucial driver of prostate cancer (PC). AR-relevant resistance remains a major challenge in castration-resistant prostate cancer (CRPC). Bromodomain and extra-terminal domain (BET) family are critical AR coregulators. Here, we developed several diphenylamine derivatives and identified compound 7d that disrupted the functions of AR and BET family in prostate cancer and exhibited favorable metabolic stability in vitro and high drug exposure in vivo. We showed 7d not only bound to AR, suppressed transactivation of wild-type AR (wt-AR) and the mutant that mediates Enzalutamide resistance, but also reduced c-Myc protein expression through BET inhibition. In addition, 7d inhibited the proliferation of AR-pos. PC cells with favorable selectivity and suppressed AR-V7-expressing VCaP and 22Rv1 xenografts growth in vivo. Collectively, these results indicate the potential of lead compound 7d as an orally available AR and BET inhibitor to treat CRPC and overcome antiandrogen resistance. This study involved multiple reactions and reactants, such as 2-Chloro-4-iodobenzonitrile (cas: 371764-70-4Application In Synthesis of 2-Chloro-4-iodobenzonitrile).
2-Chloro-4-iodobenzonitrile (cas: 371764-70-4) belongs to iodide derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Application In Synthesis of 2-Chloro-4-iodobenzonitrile
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com