Wang, Ming-bo published the artcileSynthesis and structure-activity relationship of novel tetrahydrobenzo[d]thiazole as androgen receptor modulator, Related Products of chlorides-buliding-blocks, the publication is Zhongguo Shengwu Huaxue Yu Fenzi Shengwu Xuebao (2018), 34(9), 962-971, database is CAplus.
Prostate cancer is one of the most commonly diagnosed cancer in men, and androgen receptor (AR) is an important target for the treatment of prostate cancer. For many reasons, existing AR antagonists fail to treat prostate cancer after long-term use. Therefore, the development of novel AR antagonists is still of great significance. A series of tetrahydrobenzo[d]thiazole compounds were synthesized by condensation reaction of α,β-epoxycyclohexanones and appropriate substituted thioureas 8, which were obtained from the corresponding anilines 7. Their antiandrogenic activities were tested using an yeast two-hybrid (Y2H) system, and several compounds exhibited androgen receptor (AR) antagonistic behavior equal or stronger than that of flutamide (IC50 ≤ 2.48 mmol/L). Further cell viability assay demonstrated that some active compounds effectively inhibited the proliferation of androgen-sensitive LNCaP cells values with IC50 values of 17.1-41.4 mmol/L. Mol. docking study provide a possible model of ligand receptor interactions, which was consistent with the initial structure-activity relationship (SAR) studies. Taken together, tetrahydrobenzo[d]thiazoles act as effective AR modulators may represent promising leads for further development of novel and improved AR antagonists.
Zhongguo Shengwu Huaxue Yu Fenzi Shengwu Xuebao published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C10H16Br3N, Related Products of chlorides-buliding-blocks.
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