当前位置: X-MOL 学术Chem. Data Collect. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Design, synthesis and anticancer evaluation of chalcone based thieno[2,3-d]thiazoles as anticancer agents
Chemical Data Collections Pub Date : 2021-06-23 , DOI: 10.1016/j.cdc.2021.100742
Yadaiah Sunkari , Jyothi M , Laxminarayana Eppakayala

A new series of aryl chalcone incorporated thieno[2,3-d]thiazoles (10a-j) have been designed and synthesized and their structures were confirmed by analytical data. Further, these derivatives were screened for their anticancer activity towards four human cancer cell lines such as prostate cancer (PC3), lung cancer (A549), breast cancer (MCF-7) and ovarian cancer (A2780) by employing of MTT assay. The obtained results were compared with standard drug as etoposide. Among the tested derivatives, five derivatives (10a, 10d, 10e, 10f and 10j) were revealed most promising activities Specifically, two compounds 10d (PC3=0.77±0.032 µM; A549=0.078±0.0051 µM; MCF-7 = 0.44±0.061 µM and A2780=1.46±0.92 µM) and 10e (PC3=0.03±0.0063 µM; A549=0.021±0.0075 µM; MCF-7 = 0.19±0.084 µM and A2780=0.11±0.064 µM) possessed highest anticancer activity.



中文翻译:

基于查尔酮的噻吩并[2,3- d ]噻唑作为抗癌剂的设计、合成和抗癌评价

设计并合成了一系列新的芳基查尔酮并入噻吩并[2,3- d ]噻唑(10a-j),并通过分析数据证实了它们的结构。此外,通过使用MTT测定筛选了这些衍生物对四种人类癌细胞系例如前列腺癌(PC3)、肺癌(A549)、乳腺癌(MCF-7)和卵巢癌(A2780)的抗癌活性。所得结果与标准药物如依托泊苷进行比较。在测试的衍生物中,五种衍生物(10a、10d、10e、10f10j)显示出最有希望的活性。 具体而言,两种化合物10d (PC3=0.77±0.032 µM;A549=0.078±0.0051 µM;MCF-7 = 0.414±0。 µM 和 A2780=1.46±0.92 µM) 和10e (PC3=0.03±0.0063 µM;A549=0.021±0.0075 µM;MCF-7 = 0.19±0.084 µM 和 A2780=0.11±0.064 µM) 具有最高的抗癌活性。

更新日期:2021-07-07
down
wechat
bug