Synthesis And Physiological Activity Of Aromatic Nitrogen Mustards Modified By Schiff Base

Nitrogen mustards are a sort of common chemotherapeutic agents. They have strong killing effect to various tumor cells. But as a type of alkylating agent, nitrogen mustard derivatives also contain their defects. When it inhibit and poison cancer cells, the other active normal cells may be also killed, so lots of side effects can be caused. The other, nitrogen mustards have immunosuppression effect, it can decrease our body's defense function and various infections can be caused by bacteria and virus. So how to modify nitrogen mustards'structures and decrease their side effects turn to be a research hotspot. Schiff base has been proved to have antibacterial activity and antivirus effect, especially in recent years, people found Schiff base have antitumor activity. To get new antitumor drugs which have lower side effects and higher therapeutic index, this research synthesized 16 nitrogen mustards modified by Schiff base. The contents are as follows:1. Based on largely amount literatures, this paper separately expounded the research and application of chemotherapeutic agents, nitrogen mustards and Schiff bases.2. Prepared 16 novel nitrogen mustards modified by Schiff bases via conventional heating method.3. All of the compound's structures have been characterized by IR, 1H NMR, MS.4. Studied the relationship between the temperature, the reaction time, material ratio, the structures of target compounds and yields. Give the best reaction conditions.5. Studied the Antibacterial Activity of the Schiff bases with Filter Paper Method.6. Studied the anti tumor activity in vitro of the Schiff bases with SRB Method. and MTT Method.