Synthesis And Antitumor Activity Of 1-aryl Polysubstitude Pyrrole Derivatives

Pyrrole and its derivatives are early found in bone tars and widely exist in natural animals and plants.Because of the application and the foundation domain, pyrrole and its derivatives were found and synthesized.They are widely used in pesticide, medicine, food, photographic materials and polymer materials.In recent years, research shows that many polysubstituted pyrrole and derivatives have strong biological activity especially 1-aryl substitude pyrrole have obvious biological activity in analgesic, local anesthesia. Also find that in antiphlogistic, anticancer, anti-leukemia and lowering blood pressure has the best efficiency.In this paper, we have sμMmarized the application of pyrrole derivatives in some fields, and sμMmarized the synthesis methods.We have synthesized two kinds of pyrrole derivatives by Paal-Knorr. Research and discuss the optimal conditions.14 substitude pyrrole derivatives were synthesized. Then we use MTT assay to measure the anti-proliferative effect of them on hμMan cervical carcinoma Hela cells in vitro.Content as follows:Chapter 1:The application of pyrroles and its derivatives.This chapter simply introduces the application of pyrrole and pyrrole derivatives in medicine, pesticide, biology, polymer material and photochromism.Chapter 2:Using 1-p-methylphenyl-2,5-dimethyl-3,4-diethoxycarbonyl pyrrol as the masterplate by the Paal-knorr reaction find the the optimal conditions.Chapter 3:1-aryl-substituted-2,5-dimethyl-3,4-diethoxycarbonyl pyrrol was synthesized by the Paal-knorr reaction under the optimal conditions. The products were identified by IR,1H NMR and Elemental Analysis.Chapter 4:1-aryl-substituted-2,5-dimethyl-3,4-diacetyl pyrrol was synthesized by the Paal-knorr reaction. Discuss electronic effect and spatial effect impact on the yield.Chapter 5:The anti-proliferative effect of the 14 pyrrole and derivatives on hμMan cervical carcinoma Hela cells was studied.