Structure Modifications Of Active Material In Indigo Natruralis And Study Anti-tumor Activity In Vitro

Aim:To efficient synthesis of tetrahydronaphthalene-or isochroman-fused spirooxindoles using tandem reaction with different substituted group isatin and the nitration of methyl benzene formaldehyde and evaluate pharmacologic activities of some of target compounds and their derivatives to obtain higher activity and less toxic novel spiro compounds.Methods:1. Michael-Aldol and vinylogous Henry-acetalization reaction were used to for synthesis of a series of novel quaternary carbon center, and to assemble functionalized 2-substituted tetrahydronaphthalene-or isochroman-fused spiro-oxindoles and other drug-like spirocyclic scaffolds. The structures are derived by ¹H-NMR,¹³C-NMR, HRMS, X-ray single crystal.2. Determined by MTT assay is used to target products and the derivatives of IC50 of the tumor cells.Results:1. In the process of the experiment,33 unreported new compounds were obtained. The structures of the target compounds have been comfirmed by ¹H-NMR,¹³C-NMR, HRMS analysis; 2. In vitro antitumor activity of the early screening results showed that the target products and derivatives have a certain inhibition of inhibiting tumor cells.Conclusion:The target products and its derivatives from synthese have certain anti-tumor activity.