Design and synthesis of phosphonate functionalized naphthalenediimide: Application to induce mitochondria mediated apoptosis in the human skin melanoma cells (SKMEL2)

Abstract

New phosphonate functionalized naphthalenediimides (NDI-1 and NDI-2) have been synthesized and evaluated as potential drug candidates to treat the skin malignancy. The aforementioned candidates have resulted in an induced apoptosis pathway of cytotoxicity, at concentrations lower than 4 μM, in human skin melanoma cells, and elicited a stronger apoptotic response in cells. Regulation of the Bcl2, Caspases, Bak1, Bax protein in NDI-induced apoptosis in cells has been analyzed by real time PCR, and the cell viability and apoptosis determined by flow cytometry. The obtained results indicate that NDIinduced apoptosis by regulation of Bcl2 and Bak1 occurs in human skin melanoma cells (SKMEL-2).