Evaluation of Biological Properties of Some Nitrobenzofurazan Derivatives Containing a Sulfide Group

The purpose of our study is to evaluate the antitumor activity of some previously reported nitrobenzofurazan derivatives. In this regard, their cytotoxic effect, influence on eukaryotic cell cycle, and on some genes implicated in apoptosis were evaluated. Compounds 3b, 3c and 3d induced apoptosis through both intrinsic and extrinsic pathways, while compound 3a activated only the intrinsic pathway. The most toxic derivative proved to be compound 3d; this compound also slightly increased the S phase and decreased the G0/G1 phase of the cell cycle in a dose dependent manner. Hydrophobicity (log P), polar surface area (PSA) and molecular volumes were calculated and correlated with some biological properties.