Anti-neoplastic effects of novel compounds on human head & neck squamous carcinoma cell lines

Human head and neck squamous cell carcinomas (HNSCC) are the sixth most frequent cancers worldwide, characterized by recurrent metastasis and drug resistance. Aiming to develop a different and new therapy approach, we first analysed some novel synthesized aminopyrimidine compounds on several cancer cell lines, including HNSCC. These compounds were found to be good cancer cell proliferation inhibitors, especially a N-benzyl counterpart of RDS 3442, the reference molecule that in our earlier research demonstrated to be a promising negative regulator acting on tumor cell proliferation. Afterwards we evaluated the anti-neoplastic activity of two different agents: the first one is a new synthesized molecule, named RDS 60, structurally related to nocodazole, a tubulin targeting molecule, the second one is one of the most effective kinesin Eg5 inhibitors, K858. We proved that these two compounds are potential innovative anti-tumor agents for head and neck squamous cell carcinomas. We demonstrated that both agents inhibit various malignant cancer activities, by reducing tumor cell proliferation, but not the normal somatic cell one, blocking cancer cell cycle in G2/M phase, up-regulating cyclin B1, inducing apoptotic cell death and finally reversing the epithelial- mesenchymal transition, cell motility and extracellular matrix invasion in HNSCC.