Synthesis and Anticancer Activity of 1,5-Disubstituted Isatin Derivatives
|School||East China University of Science and Technology|
|Course||Pharmaceutical Engineering and Technology|
|Keywords||Synthesis 1,5-disubstituted isatin derivatives MTT assay Anticancer activity|
Isatin is an endogenous compound, which is widely used in chemical industry and medical industy due to its excellent chemical and physical properties. As reported, isatin and its derivatives possess good antitumor activity, antibacterial activity, antifungal activity, antiviral activity, anti-HIV activity and antivirus activity. Their application in central nervous system has also been intensively studied.In this thesis,1,5-disubsitituted isatin derivatives, including 1-phenzyl-5-bromo-indoline-2,3-dione, 1-phenzyl-5-chloroindoline-2,3-dione, 1-phenzyl-5-nitro-indoline-2,3-dione, and 1-phenzyl-5-(N,N-diacetylamino)indoline-2,3-dione, have been synthesized. All these compounds were identified by IR,1HNMR, MS and HRMS spectras.These isatin derivatives were also evaluated for anticancer activities against human breast cancer cell lines (MCF-7), non small cell lung cancer cell lines (A549), ovarian cancer cell strain cell lines (Skov3), cutaneous squamous cell lines (A431), human colon cancer cell lines (SW480), uterine cervical cancer cell lines (Hela), human hepatoma cell lines (HepG2) and human gastric carcinoma cell lines (MNK-45) by MTT assay. These compounds have shown inhibition against these cancer cells growth to some extent.5-(N,N-diacetylamino) isatin analogs gained by reduction and acylation, particularly, were the most potent series towards these cancer cell lines. This work will be benefit for future study to elaborate more potent anticancer istain derivatives.