A Novel Quinazoline Antitumor Drugs Of Synthetic Process And Research

The epidermal growth factor tyrosine kinase plays a very important role in the process of tumor generation. It is mainly caused by receptor phosphorylated which activates cell proliferation. Therefore, epidermal growth factor receptor has become a new target of tumor treatment. The epidermal growth factor inhibitor most of which are designed on the basis of quinazoline, such as gefitinib, erlotinib and so on, are clinically proven that have good antitumor activity.According to analysising of the efficacy of quinazoline ring system structure, we come up with a novel quinazoline compounds on the basis of 4-amino quinazoline skeleton. Because the quinazoline structure is necessary and important of the pharmacological activity, therefore, the renovation is mainly on 4,6and 7 sites. Moreover, we have simulated the compounds activity which we designed, and the results showed that they all have a very good active effect.After complete chemical synthesis of the compounds we designed,we will get a series of specific chemical compounds which can inhibit tyrosine kinase.Then through the activity and toxicity text, we can get some antitumor compounds which have more activity and less toxicity. In addition, because aza-crown ethers have their unique properties, the left side of the ring system modification could increase a new potential targets which will make the compound have more target ability. To sum up, we will expect to get some new antitumor compounds which have more target ability, more activity and less toxicity.