3-硝基-4-色满酮衍生物作为去势抵抗性前列腺癌潜在抗增殖剂的合成及生物学评价

Synthesis and biological evaluation of 3-nitro-4-chromanone derivatives as potential antiproliferative agents for castration-resistant prostate cancer.

作者信息

Chen Huiqing, Xing Yajing, Xie Jia, Xie Jiuqing, Xing Dong, Tang Jie, Yang Fan, Yi Zhengfang, Qiu Wen-Wei

机构信息

Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University Shanghai 200062 China

Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University Shanghai 200241 China

出版信息

RSC Adv. 2019 Oct 21;9(58):33794-33799. doi: 10.1039/c9ra06420f. eCollection 2019 Oct 18.

A series of novel 3-nitro-4-chromanones were synthesized and their cytotoxicity was evaluated on castration-resistant prostate cancer cell (CRPC) lines using the sulforhodamine B (SRB) assay. The amide derivatives showed more potent antitumor activity than their corresponding ester derivatives. Most of the tested compounds showed less toxicity towards human fibroblasts (HAF) compared with the tumor cell lines. The optimal compound 36 possessed much more potent antiproliferative activity than the positive compound cisplatin. The colony formation, cell cycle distribution, apoptosis, transwell migration and wound healing assays of 36 were performed on CRPC cell lines.