新型β-咔啉-3-(4-亚苄基)-4H-噁唑-5-酮衍生物的合成与抗肿瘤活性评价。
Synthesis and evaluation of new β-carboline-3-(4-benzylidene)-4H-oxazol-5-one derivatives as antitumor agents.
机构信息
Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Maringá, Av. Colombo, 5790, Maringá, 87020-900 PR, Brazil.
出版信息
Molecules. 2012 May 21;17(5):6100-13. doi: 10.3390/molecules17056100.
In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-β-carbolin-3-yl]-4-(benzylidene)-4H-oxazol-5-one (11) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC50 values of 0.48, 1.50 and 1.07 µM, respectively. An in silico study of the ADME properties of the novel synthesized β-carboline derivatives was also performed.
在本工作中，我们报道了一系列新型 1-取代-β-咔啉衍生物的合成及体外抗肿瘤和抗菌活性评价，这些衍生物在 C-3 位上带有 4-亚苄基-4H-噁唑-5-酮单元。化合物 2-[1-(4-甲氧基苯基)-9H-β-咔啉-3-基]-4-(亚苄基)-4H-噁唑-5-酮（11）是最具活性的衍生物，对神经胶质瘤（U251）、前列腺（PC-3）和卵巢（OVCAR-03）癌细胞系表现出很强的细胞毒性，IC50 值分别为 0.48、1.50 和 1.07µM。还对新型合成的β-咔啉衍生物的 ADME 性质进行了计算研究。
Zotero 插件