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Chromene, Quinoline Hybrids as Potential Anti-Cancer Agents: A Novel and Distinct Approach for the Synthesis of Quinoline Derivatives
Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2021-03-31 , DOI: 10.2174/1570178617666200122095829
Rizuana Sultana 1 , Ravinder Reddy Tippanna 1
Affiliation  

A series of novel quinoline derivatives (6-phenyl-6H-chromeno[4,3-b]quinoline) have been prepared by using 4-chloro-2-phenyl-2H-chromene-3-carbaldehyde and various substituted isocyanides as starting materials in the presence of HClO4-SiO2 and Methanol. We screened eighteen compounds of this novel series (6a-r) in six different cancer cell lines (A549 (lung cancer cells), DU145 (prostate cancer cells), PC3 (prostate cancer cells), MCF7 (lung cancer cells), HT 29, HCT 116 (colon cancer cells). Most of the compounds showed anti-cancer activity and compound 6b showed good cytotoxicity IC50 = 2.61±0.34 μM against colon cancer on HT29 cell line among all. The key property of cell migration was observed while treatment cells with 6b. Apoptosis in HT29 cells confirmed by annexin V staining, acridine orange/ethidium bromide (AO/EB), DAPI, induced by 6b. This method is operationally simple and works with a diverse range of substrates. These results indicate the anticancer potential of these series and warrants future investigations for further anticancer drug development.



中文翻译:

铬,喹啉杂化物作为潜在的抗癌剂:一种新颖独特的方法合成喹啉衍生物。

以4-氯-2-苯基-2H-色烯-3-甲醛为起始原料,制备了一系列新颖的喹啉衍生物(6-苯基-6H-chromeno [4,3-b]喹啉)。在HClO 4 -SiO 2存在下和甲醇。我们在六种不同的癌细胞系(A549(肺癌细胞),DU145(前列腺癌细胞),PC3(前列腺癌细胞),MCF7(肺癌细胞),HT 29)中筛选了18个此新系列化合物(6a-r) ,HCT 116(结肠癌细胞);大多数化合物对HT29细胞系均具有抗癌活性,化合物6b对结肠癌具有良好的细胞毒性IC50 = 2.61±0.34μM,观察到细胞迁移的关键特性6b诱导的HT29细胞凋亡,通过膜联蛋白V染色,a啶橙/溴化乙锭(AO / EB),DAPI的6b诱导证实,该方法操作简便,可用于多种底物,这些结果表明该药物具有抗癌作用这些系列的潜力,并有待进一步研究开发抗癌药物。

更新日期:2021-03-31
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