کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1392825 | 1501161 | 2012 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents](/preview/png/1392825.png)
A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a–v were prepared and studied for their anticancer activity against selected human cancer cell lines. The reaction of indolylhydrazides 3a–h with a variety of aryl isothiocyanates 4 afforded the key intermediate thiosemicarbazides 5a–v, which upon treatment with acetyl chloride produced the 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a–v in good yields. Most of the synthesized compounds showed selective cytotoxicity towards human breast cancer cell line (MDA-MB-231). Of the synthesized 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles, compound 6f is the most potent towards tested cancer cell lines (IC50 = 0.15–1.18 μM).
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► Diverse series of novel 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles were synthesized.
► All the compounds were evaluated for their in-vitro anticancer activity.
► The compounds are selective against MDA-MB-231 cancer cell line (IC50 < 1 μM).
► The most potent compound showed IC50 value of 150 nM against LnCap cancer cell line.
Journal: European Journal of Medicinal Chemistry - Volume 55, September 2012, Pages 432–438