Antitumor Activity of PEGylated and TEGylated Phenothiazine Derivatives: Structure-Activity Relationship

The paper aims to investigate the antitumor activity of a series of phenothiazine derivatives in order to establish a structure-antitumor activity relationship. To this end, PEGylated and TEGylated phenothiazine have been functionalized with formyl units and further with sulfonamide units via dynamic imine bonds. Their antitumor activity was monitored in vitro against seven human tumors cell lines and a mouse one compared to a human normal cell line by MTS assay. In order to find the potential influence of different building blocks on antitumor activity, the antioxidant activity, the ability to inhibit farnesyltransferase and the capacity to bind amino acids relevant for tumor cell growth were investigated as well. It was established that different building blocks conferred different functionalities, inducing specific antitumor activity against the tumor cells.

Automated summary

The aim of this study is to investigate the antitumor activity of phenothiazine derivatives and establish a structure-antitumor activity relationship. PEGylated and TEGylated phenothiazine were functionalized with formyl units and further with sulfonamide units using dynamic imine bonds. Their antitumor activity was tested in vitro against human and mouse tumor cell lines, and the potential influence of different building blocks on antitumor activity was explored.