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Short Paper | Regular issue | Vol 91, No. 3, 2015, pp.583-592
Published online, 30th January, 2015
DOI: 10.3987/COM-14-13146
Synthesis and Antitumor Activity of 1,3,4-Thiadiazole Derivatives Bearing Coumarine Ring

Sobhi M. Gomha* and Hassan M. Abdel-aziz

*Department of Organic Chemistry, Cairo University, Giza-Haram 12613, Egypt


In the present study, preparation of a novel series of N'-(3,5-diphenyl-1,3,4-thiadiazol-2(3H)-ylidene)-2-oxo-2H-chromene-3-carbohydrazide (8a-m) was prepared by two methods via the reaction of hydrazonoyl halides with methyl 2-(2-oxo-2H-chromene-3-carbonyl)hydrazinecarbodithioate or 3-(5-mercapto-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one. Structures of the newly synthesized compounds were elucidated on the basis of elemental analyses and spectral data. All the newly synthesized compounds have been evaluated for their antitumor activity against a liver carcinoma cell line HEPG2-1. Also, their structure activity relationship (SAR) was studied. Many of the tested compounds showed moderate to high anticancer activity with respective to doxorubicin as a reference drug.