α-苯乙胺二茂铁羧酸共晶体的抗癌活性研究

IF 2.8 4区 化学 Q2 CHEMISTRY, ANALYTICAL
Chirality Pub Date : 2024-02-25 DOI:10.1002/chir.23653
Liao Youyin, Ma Yuexing, Chen Jiahao, Qian Kun, Yang Jie, Pan Rongbin, Xu Yiyong
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引用次数: 0

摘要

二茂铁衍生物在医学领域,特别是抗肿瘤领域显示出广泛的药理活性,可作为治疗肿瘤和其他疾病的候选药物或先导化合物。α-苯乙胺是制备精细化工产品的重要中间体。(R)-(+)-1-苯乙胺二茂铁羧酸/(S)-(-)-1-苯乙胺二茂铁羧酸分别被命名为化合物 1 和 2。单晶 X 射线衍射显示,化合物 1 和 2 结晶为正方晶系空间群 P212121,且化合物 1 和 2 的晶体结构呈镜像对称。MTT 比色法检测了两种化合物对 SW480、MDA-MB-231 和 H1299 细胞的抑制作用。同时还计算了化合物对癌细胞的 IC50 值。S构型化合物的抗癌效果更为明显。化合物 2 能使野生型癌细胞凋亡,从而预防癌症;它还具有帮助细胞修复基因缺陷的功能。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Study on the anti-cancer activity of α-phenethylamine ferrocenecarboxylic acid co-crystals

Study on the anti-cancer activity of α-phenethylamine ferrocenecarboxylic acid co-crystals

Study on the anti-cancer activity of α-phenethylamine ferrocenecarboxylic acid co-crystals

Ferrocene derivatives show a wide range of pharmacological activities in the medical field, especially in the anti-tumor field, and can be used as candidate drugs or lead compounds for the treatment of tumors and other diseases. And α-phenethylamine is an important intermediate for the preparation of fine chemical products. (R)-(+)-1-Phenethylamine ferrocenecarboxylic acid/(S)-(−)-1-phenethylamine ferrocenecarboxylic acid were prepared, named compounds 1 and 2, respectively. Single crystal X-ray diffraction showed that compounds 1 and 2 crystallized in the orthorhombic system space group P212121, and the crystal structures of compounds 1 and 2 exhibited mirror symmetry. The inhibitory effect of two compounds on SW480, MDA-MB-231, and H1299 cells was tested by MTT colorimetry. The IC50 values of the compounds against cancer cells were also calculated. The anti-cancer effect was more pronounced for compounds in the S-configuration. Compound 2 made the wild-type cancer cells undergo apoptosis, thus preventing cancer; it also had the function of helping the cell gene repair defects.

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来源期刊
Chirality
Chirality 医学-分析化学
CiteScore
4.40
自引率
5.00%
发文量
124
审稿时长
1 months
期刊介绍: The main aim of the journal is to publish original contributions of scientific work on the role of chirality in chemistry and biochemistry in respect to biological, chemical, materials, pharmacological, spectroscopic and physical properties. Papers on the chemistry (physiochemical, preparative synthetic, and analytical), physics, pharmacology, clinical pharmacology, toxicology, and other biological aspects of chiral molecules will be published.
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