Synthesis of a New Pyridine Pharmaceutical Intermediate in Potential Anti-cancer of HDACI

Abstract

In order to obtain better anti-cancer activity of HDACI, new HDCIs analog and a pyridine pharmaceutical intermediate were designed by comparing the molecule of FK228 and Largazole and introducing the pyridine intermediate to the cyclic tetrapeptide pharmacophore. The synthetic route of HDCIs analog and the pyridine intermediate were designed. The HDCIs analog and the pyridine intermediate were all synthesized, and the optimum conditions of synthesizing the pyridine intermediate were got by using parallel test. The pyridine intermediate can be used to manufacture new potential HDACIs by forming new structure of the polypeptide. Due to the special structure of the pyridine intermediate, it can also be widely used in other medical field. Through our work we have designed synthetic routes of the pyridine intermediate and discussed the optimum conditions. And we provide a new synthesis method of cyclopeptide HDCIs.