一些isatin-linked chalcones作为新型抗乳腺癌药物的设计、合成和生物学评价:分子杂交方法

Chandrabose Karthikeyan , Viswas Raja Solomon , Hoyun Lee , Piyush Trivedi
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引用次数: 47

摘要

Isatins是存在于人类和哺乳动物体内的内源性分子,具有多种药理特征,包括抗癌活性。类似地,查尔酮是许多天然产物中常见的亚结构,属于类黄酮家族,显示出有效的抗癌特性。设计并合成了一种新的3-(2-氧-2-苯基乙基)吲哚-2-酮类化合物,该化合物含有鸢尾素和查尔酮的药效成分。这些化合物对三种乳腺癌细胞系的抗癌活性进行了评估。大多数化合物显示出良好的抗癌活性(<20 μM)。化合物2c对MDA-MB231、MDA-MB468和MCF7细胞的GI50值分别为8.54、4.76和3.59,是该系列中活性最高的化合物,其isatin部分的苯环上有一个5-氯取代,苯基环上有3,4-二甲氧基取代。总的来说,这项研究的发现突出了3-(2-氧-2-苯基乙基)吲哚-2- 1作为寻找治疗乳腺癌药物的潜在新先导。
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Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach

Isatins are endogenous molecules present in human and mammals which exhibits diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures in numerous natural products belonging to the flavonoid family, show potent anticancer properties. A novel series of 3-(2-oxo-2-phenylethylidene)indolin-2-ones incorporating pharmacophoric elements of isatins and chalcones were designed and synthesized. The compounds were evaluated for anticancer activity against three breast cancer cell lines. Most of the compounds showed promising anticancer activity (< 20 μM) against the studied cell lines. Compound 2c, bearing a 5-chloro substituent in the benzo ring of the isatin moiety and 3,4-dimethoxy substitutions in the phenyl ring, was found to be the most active in the series with GI50 values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF7 cells, respectively. Overall, the findings of the study highlight 3-(2-oxo-2-phenylethylidene)indolin-2-one as a potential new lead in the search of drugs for the treatment of breast cancer.

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