Intended To Colchicine Compound Synthesis And Antitumor Activity Of Research

Cancers are one kind of familiar and important diseases which threaten human health. Chemical drugs occupied important position in the treatment of cancer. Colchicine is a well known anti-gout drug, its clinical application has more than 200 years. In 1970s, this drug is part of the success for the treatment of tumors. In recent years, with its in-depth pharmacological studies, It was reported that colchicine interferes with microtubule growth, therefore, affects mitosis and other microtubule dependent functions.Colchicine composed by three ring skeleton. Inspired by the special structure and biological activity, the new derivatives with similar skeleton were designed synthesized with two synthetic routes.In route 1, the first step, nine chalcone were synthesized by the condensation of substituted benzaldehydes and substituted acetophenone. Then three dihydrochalcones were synthesized through chalcone hydrogenation, The method was very convenient and the all yields were over 80%.The third step, intra-molecular ring close to form colchicine derivatives from dihydrochalcone were not succeeded.In route 2, the first step, six nitrostyrenes were synthesized by the condensation of substituted benzaldehydes and nitromethane. Then in the second step, the Michael addition of substituted acetophenone to nitrostyrene were explored, but not succeeded.All structures of synthetic compounds were confirmed by 1HNMR. The anti-tumor activity was assayed by MTT method. The results showed that the synthetic intermediates of colchicines no anti-tumor activity. That implies tricycle structure is necessary motif.