synthesis and anticancer activity of some new s-glycosyl and s-alkyl 1,2,4-triazinone derivatives合成和抗癌活性的一些新的s-glycosyl s-alkyl 1,2,4-triazinone衍生品.pdfVIP

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synthesis and anticancer activity of some new s-glycosyl and s-alkyl 1,2,4-triazinone derivatives合成和抗癌活性的一些新的s-glycosyl s-alkyl 1,2,4-triazinone衍生品.pdf

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synthesis and anticancer activity of some new s-glycosyl and s-alkyl 1,2,4-triazinone derivatives合成和抗癌活性的一些新的s-glycosyl s-alkyl 1,2,4-triazinone衍生品

Molecules 2011, 16, 5682-5700; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Anticancer Activity of Some New S-Glycosyl and S-Alkyl 1,2,4-Triazinone Derivatives Hosam A. Saad 1,2,* and Ahmed H. Moustafa 2 1 Department of Chemistry, Faculty of Science, Taif University, Taif, 21974, Kingdom of Saudi Arabia 2 Department of Chemistry, Faculty of Science, Zagazig University, Zagazig, 44511, Egypt * Author to whom correspondence should be addressed; E-Mail: h_saadzag@; Tel.: +96-65-5342-0899; +20-10-537-3242; Fax: +20-55-228-5374. Received: 31 May 2011; in revised form: 27 June 2011 / Accepted: 29 June 2011 / Published: 4 July 2011 Abstract: A series of S-glycosyl and S-alkyl derivatives of 4-amino-3-mercapto-6-(2-(2- thienyl)vinyl)-1,2,4-triazin-5(4H)-one (1) were synthesized using different halo compounds such as preacetylated sugar bromide, 4-bromobutylacetate, 2-acetoxyethoxy- methyl bromide, 3-chloropropanol, 1,3-dichloro-2-propanol, epichlorohydrin, allyl bromide, propargyl bromide, phthalic and succinic acids in POCl3. The structures of the synthesized compounds have been deduced from their elemental analysis and spectral (IR, 1H-NMR, and 13C-NMR) data. Some of the synthesized compounds were screened as anticancer agents. Significant anticancer activities were observed in vitro for some members of the series, and compou