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Study on the anti‐cancer activity of α‐phenethylamine ferrocenecarboxylic acid co‐crystals
Chirality ( IF 2 ) Pub Date : 2024-02-26 , DOI: 10.1002/chir.23653
Liao Youyin 1 , Ma Yuexing 1, 2, 3 , Chen Jiahao 1 , Qian Kun 1 , Yang Jie 1 , Pan Rongbin 4 , Xu Yiyong 5
Affiliation  

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.

中文翻译:

α-苯乙胺二茂铁甲酸共晶的抗癌活性研究

二茂铁衍生物在医学领域,尤其是抗肿瘤领域表现出广泛的药理活性,可作为治疗肿瘤等疾病的候选药物或先导化合物。和α‐苯乙胺是制备精细化工产品的重要中间体。()-(+)-1-苯乙胺二茂铁甲酸/(S制备了)-(-)-1-苯乙胺二茂铁甲酸,分别命名为化合物1和2。单晶X射线衍射表明化合物1和2结晶于斜方晶系空间群212121,化合物1和2的晶体结构呈镜面对称。采用MTT比色法检测两种化合物对SW480、MDA-MB-231和H1299细胞的抑制作用。集成电路50还计算了化合物对抗癌细胞的值。化合物的抗癌作用更为明显S-配置。化合物2使野生型癌细胞发生凋亡,从而预防癌症;它还具有帮助细胞基因修复缺陷的功能。
更新日期:2024-02-26
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