Letters in Organic Chemistry ( IF 0.8 ) Pub Date : 2020-10-31 , DOI: 10.2174/1570178617666200225102939 Shaik Shahinshavali 1 , Nuthalapati Poojith 2 , Venkat Rao Guttikonda 3 , Reddymasu Sreenivasulu 4 , Mandava Venkata Basaveswara Rao 1
We have synthesized a library of new 1,2,3-triazole incorporated 1,3,4-thiadiazoleisothiazolo[ 4,3-b]pyridine derivatives 12a-j and have screened these products for their anticancer activities against four human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer), and MDA MB-231 (breast cancer) using MTT assay with etoposide as a positive control. Among them, compound 12e has shown excellent activities against MCF-7, A549, DU-145, and MDA-MB-231 with IC50 values of 0.53±0.055 μM, 0.18±0.077 μM, 0.10±0.082 μM, and 0.92±0.041 μM, respectively.
中文翻译:
1,2,3-三唑,1,3,4-噻二唑和异噻唑并[4,3-b]吡啶环的乙酰胺的设计,合成及抗癌评估
我们合成了一个新的1,2,3-三唑并入1,3,4-噻二唑异噻唑并[4,3-b]吡啶衍生物12a-j的文库,并筛选了这些产品对四种人类癌细胞系的抗癌活性。使用依托泊苷作为阳性对照的MTT分析检测MCF-7(乳腺癌),A549(肺癌),DU-145(前列腺癌)和MDA MB-231(乳腺癌)。其中,化合物12e对MCF-7,A549,DU-145和MDA-MB-231具有优异的活性,IC50值分别为0.53±0.055μM,0.18±0.077μM,0.10±0.082μM和0.92±0.041μM , 分别。