Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer was written by Yu, Jiang;Zhang, Lanxi;Yan, Guoyi;Zhou, Peiting;Cao, Chaoguo;Zhou, Fei;Li, Xinghai;Chen, Yuanwei. And the article was included in European Journal of Medicinal Chemistry in 2019.Quality Control of 2-Chloro-4-iodobenzonitrile The following contents are mentioned in the article:
Prostate cancer (PC) is the second most common malignancy in men worldwide. Among current therapies, two antiandrogens, Abiraterone Acetate and Enzalutamide (Enza) have become the standard of care for patients with metastatic castration-resistant prostate cancer (mCRPC). Here, the authors designed and synthesized a new series of nonsteroidal compounds deriving from the hybridization of Abiraterone (Abi) and Enzalutamide, among which compound I featuring the diphenylamine scaffold was identified as a potent and cell selective androgen receptor (AR) antagonist. In cell proliferation assays, compound I exhibited better antiproliferative activities than Enzalutamide against AR-overexpressing VCaP cells and 22Rv1 cells bearing H874Y-mutated AR. In addition, I suppressed the activity of AR-F876L mutant that confers resistance to Enzalutamide and efficiently blocked R1881-induced PSA and FKBP5 gene expression. In competitive binding assay, compound I displayed higher binding affinity to AR than Enzalutamide. These results suggest compound I as a potential candidate to treat Enza-resistant CRPC. This study involved multiple reactions and reactants, such as 2-Chloro-4-iodobenzonitrile (cas: 371764-70-4Quality Control of 2-Chloro-4-iodobenzonitrile).
2-Chloro-4-iodobenzonitrile (cas: 371764-70-4) belongs to iodide derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Quality Control of 2-Chloro-4-iodobenzonitrile
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com