Synthesis and Antitumor Activity Evaluation of 3,6-Substituted- 1,2,4-triazolo[3,4-a]phthalazine Derivatives

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With the aim of obtaining potential antitumor candidates with more efficiency and more economic value. A series of 3,6-substituted-1,2,4-triazolo(3,4-a)phthalazine derivatives were synthesized. The target products were obtained via cycliza- tion, chlorination, substitution, cyclization, substituted with phthalic anhydride used as the starting material. The structures of target products are confirmed by 1 H NMR, I3 C NMR, HRMS. A series of 3,6-substituted-1,2,4-triazolo(3,4-a) phthalazine de- rivatives was evaluated for anticancer activity on four human cancer cell lines including EC-9706, HeLa and MCF-7 by MTT assay. Among them, compound 5d was more cytotoxic against EC-9706 and HeLa cell lines, with IC50 values ranging from 3.9 to 4.5 µmolL -1 , which are superior or comparable to 5-Fuorouracil. Flow cytometry analysis indicated that compound 5d

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