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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.

DOI:10.1039/c9ra06420f
PMID:35528914
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9073653/
Abstract

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.

摘要

合成了一系列新型3-硝基-4-色满酮，并使用磺酰罗丹明B（SRB）测定法在去势抵抗性前列腺癌细胞（CRPC）系上评估了它们的细胞毒性。酰胺衍生物显示出比其相应的酯衍生物更强的抗肿瘤活性。与肿瘤细胞系相比，大多数测试化合物对人成纤维细胞（HAF）的毒性较小。最佳化合物36比阳性化合物顺铂具有更强的抗增殖活性。在CRPC细胞系上对36进行了集落形成、细胞周期分布、凋亡、Transwell迁移和伤口愈合测定。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/751c013f5941/c9ra06420f-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/7ded3afd083a/c9ra06420f-f1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/675a8d4b5e07/c9ra06420f-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/4bbc310c05c5/c9ra06420f-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/333fc67d4e50/c9ra06420f-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/751c013f5941/c9ra06420f-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/7ded3afd083a/c9ra06420f-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/cd80d79a1ead/c9ra06420f-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/675a8d4b5e07/c9ra06420f-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/4bbc310c05c5/c9ra06420f-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/333fc67d4e50/c9ra06420f-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/42b7/9073653/751c013f5941/c9ra06420f-f5.jpg

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