3,6-取代-1,2,4-三氮唑[3,4- a ]酞嗪衍生物的合成和抗肿瘤活性评价

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