Highly efficient antitumor agents of heterocycles containing sulfur atom: Linear and angular thiazonaphthalimides against human lung cancer cell in vitro Original Research Article

A novel series of aminothiazonaphthalimides, A1–2 and B1–2, has been regioselectively synthesized. The linear compounds B1–2 were evaluated to be far more active than their angular isomers A1–2 in antitumor evaluation. The linear compounds C–F, derived from compound B1, all showed highly efficient antitumor activities against A549 and P388 cell lines. Also, cytotoxicities of these four analogues against two tumor cells were highly dependent on the length of the side chains. The compound A1 or B1, with two methylene units in the side chain, was more cytotoxic than its corresponding homologue A2 or B2, with one more methylene unit.