Design,Synthesis And Evaluation Of Novel Flavonoids And Imides Derivatives Containing Naphthyl

Naphthalene with a rigid planar ring and a wide range of biological activities has been used in material preparation,pharmaceutical development,agricultural production.Especially in drug research and development,naphthalene is often used as a pharmacophore or privileged fragment.Flavonoids and naphthalimides show potent anti-tumor activity,and have been considered as research hotspots in the medicinal field.And some related flavonoid and naphthalimide derivatives are undergoing clinical trials.First,compounds ZX-A-01 and ZX-B-01 with significant antitumor activity were previously synthesized by our Lab.in a low yield.In order to obtain enough compounds for further research,the synthesis condition of ZX-A-01 and ZX-B-01 was optimized respectively.The total yields were elevated to the gram-scale by screening synthesis condition.Five novel relevant flavonoid derivatives were also prepared by the modified route.Second,with acenaphthene as the starting material,18 novel naphthalimide derivatives modified with bromine,cyan and nitrogen heterocycle fragments were designed and synthesized.The target compounds were evaluated for their anti-proliferation activity in vitro by MTT assays against HepG2,HCT-116 and SMMC-7721 cell lines.The results showed that some novel naphthalimide derivatives exhibited significant antitumor activity with IC₅₀0 values of less than 10mmol/L.The structure-activity relationships revealed that the presence of pyrimidine fragment is beneficial for the antitumor activity.