Atovaquone analogues Design, Synthesis and antitumor activity of
|School||Nanjing Normal University|
|Course||Microbial and Biochemical Pharmacy|
|Keywords||Atovaquone design and synthesis of derivatives structure confirmation anti-tumor activity|
Malignant tumor has been endangering people’s health. According to statistics of WHO, the number of people, who were dead because of malignant tumor, reaches 9.6 million in 5 billion people of the world every year, even is increasing year after year. So every country is attaching importance to the study of tumor and anti-tumor drugs at all times, and have taken out great progress.In the study, atovaquone was chosen as the lead compounds. According to its structure and mechanism of action, while retaining the 1,4-naphthoquinone structure, we had done some new design, and opened up the corresponding synthetic route. Take 1,4-naphthoquinone, piperazine and halogenatedaromatics as raw material, we had obtained 10 new target compounds which had no literature reports through Ullman and Michael addition reaction. The chemical structure of the target compounds were determined by using HNMR, IR, MS analysis and other modern equipment means.Adopted Dul45 (people prostate cancer cells for the synthesis of goal) cell, and taked Doxorubicin as the positive control, we carried on the preliminary research of the antitumor activity of the 10 new target compounds. It is showed that:part of the target compounds appeared good antitumor activity.