- A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents
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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).
- Kumar, Dalip,Kumar, N. Maruthi,Noel, Brett,Shah, Kavita
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p. 432 - 438
(2012/11/07)
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- SYNTHESIS AND PROPERTIES OF AZOLES AND THEIR DERIVATIVES. 36. SYNTHESIS OF 2-AMINO-1,3,4-OXADIAZOLES, 2-AMINO-1,3,4-THIADIAZOLES, AND 1,2,4-TRIAZOLINE-3-THIONES CONTAINING INDOLYL RADICALS
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On the heterocyclization of 1-(indol-3-ylcarbonyl)thiosemicarbazides, depending on the conditions of performing the reaction, either 1,2,4-triazoline-3-thiones, 2-amino-1,3,4-thiadiazoles, or 2-amino-1,3,4-oxadiazoles containing an indolyl residue in posi
- Kelarev, V. I.,Shvekhgeimer, G. A.,Lunin, A. F.
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p. 1043 - 1048
(2007/10/02)
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