α-三氟甲基查耳酮作为潜在的雄激素受体非依赖性前列腺癌抗癌剂。

School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Science, Kanazawa University, Kanazawa 920-1192, Japan.

Department of Integrative Cancer Therapy and Urology, School of Medical Sciences, Kanazawa University, Kanazawa 920-1192, Japan.

Molecules. 2021 May 10;26(9):2812. doi: 10.3390/molecules26092812.

α-Trifluoromethyl chalcones were prepared and evaluated for their antiproliferative activities against androgen-independent prostate cancer cell lines as well as five additional types of human tumor cell lines. The most potent chalcone showed superior antitumor activity in vivo with both oral and intraperitoneal administration at 3 mg/kg. Cell-based mechanism of action studies demonstrated that induced cell accumulation at sub-G1 and G2/M phases without interfering with microtubule polymerization. Furthermore, several cancer cell growth-related proteins were identified by using chalcone as a bait for the affinity purification of binding proteins.

α-三氟甲基查耳酮被制备并评价其对雄激素非依赖性前列腺癌细胞系以及另外五种人类肿瘤细胞系的抗增殖活性。最有效的查尔酮在 3mg/kg 的口服和腹腔内给药时在体内显示出优越的抗肿瘤活性。基于细胞的作用机制研究表明，诱导细胞在 sub-G1 和 G2/M 期积累，而不干扰微管聚合。此外，使用查尔酮作为结合蛋白亲和纯化的诱饵，鉴定了几种与癌细胞生长相关的蛋白质。