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Syntheses and antitumor activity of some 1,2,4 – triazine derivatives

Abstract

The 2,3,5- tri substituted –1,2,4triazin -6 - ones (2,3) are synthesized via condensation of 2- phenyl - 4 - (4- Floro benzylidene) 1,3-oxazol -5- one (1) with hydrazine hydrate, semicarbazide, and thiosemicarbazide, followed by cyclization with removal of water molecule. Acetylating compounds 2,3 with acetic anhydride yields the diacetyl derivative 4 and fused triazolo - 1,2,4triazine derivative 5, respectively. Treatment of compound 3a with ethyl chloro acetate in the presence of fused sodium acetate gives the corresponding fused 1,2,4-triazine derivative 6. 3- acetyl- 5,5- di substituted -1,2-dihydro - 1,2,4- triazino-1,2,4-triazin - 1,4,8-triones 7 was prepared via acetylating compound 6 with acetic anhydride under reflux. The structure of the compounds were characterized based on their spectral data. The cyotoxic activities of the prepared compounds have been studied on the tumor cell line human colon carcinoma (HCT- 116) cell using the MTT viability test.

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