Synthesis and Antitumor Activity of an Analog of Phthalascidin

An analog of phthalascidin (Pt-650) was synthesized with an improved synthetic route.With precursor 2 as the starting material, compound 1 was prepared through 4 steps in a total yield of 47%. In vitro antitumor test of this Pt-650 analog showed that it possessed strong toxicity against a number of tumor cell lines including A2780, A549, Bel-7402, BGC-823, HELA, KB,KeTr3 and HCT-8.