Synthesis And Biological Activity Of 2,3-substituted Indole Derivatives

Indole derivatives have attracted a great deal of attention for the some reasons that indole ring structure is similar to purines structure in DNA.And distinct molecular skeleton structure can be modified by the pharmacophore of different properties,producing various biological activities,such as anti-tumor,anti-bacterial.Their molecular design,synthesis and biological activity research were a focus of the resesrch and development of creating new drug molecular.This paper reviewed the discovery of indole derivatives,also summarized in detail the recent development of derivatives taking indole as pharmacophore.On this basis,to find new indole derivatives with highly effective activity,the molecular structure with biological activity was introduced into the structure of indole by the molecular design theory and joining principle of biological active,synthesizing 31new 2,3-substituted indole derivatives from the two series of 7a-7s and 8a-8l.In my paper,all of the target compounds were characterized by ¹H NMR?¹³C NMR?HRMS.The turbidity method was used to test the antibacterial activity of the target compounds.The antibacterial result of the target compounds 7a-7s and 8a-8l showed that the compounds 7a-7s showed good inhibitory activity against X.oryzae,and relatively low inhibitory activities against X.citri and R.solanacearum.Compounds 7b,7c,7e,7f,7g,7m,7p,7q,7r inhibited X.oryzae in vitro with EC₅₀values of 18.28,67.20,47.86,63.09,12.21,70.79,34.30,36.88 and 20.25?g/mL,respectively,which were superior to those of bismerthiazol?92.23?g/mL?.Compounds 8d,8e,8i,8k,8l displayed significant antibacterial activities?100%?against X.oryzae and R.solanacearum at a concentration of 100?g/mL.Especially,compounds 8e and 8l shown excellent antibacterial activities with EC₅₀0 values of13.70 and 16.98?g/mL,9.12 and 13.67?g/mL against X.oryzae and R.solanacearum,respectively,which were superior to the commercial antibacterial agent bismerthiazol?91.21 and 58.88?g/mL?.The antitumor activity of the target compounds 7a-7s was evaluated by MTT colorimetric method.The result showed that the inhibitory activity of target compound 7h against human cervical cancer cells?HeLa?was 100%at the agent concentration of 50?M.The inhibitory activities of the other compounds against human cervical cancer cells were weaker than that of the control drug gefitinib?100%?.The target compounds 7a-7s shown no anticancer activity against human hepatoma cells?HepG2?.