Synthesis of new phosphate derivative of benzothiazole and its inhibiting effect on two series of human neuroblastoma cell growth

摘要

The sodium salt of di ((1-hydroxy-2-benzothiazolium-1-yl) ethyliden-1,1-H-bisphosphonic acid) ortho-phosphate was synthesized and its toxicity and viability effects screened on two different human neuroblastoma cell lines. This novel derivative of benzothiazole provides a new compound in connection with research and therapeutic application for tumor cell growth inhibition. Benzothiazole was alkylated in reaction with bromoacetic acid and then converted to its H-bisphosphonic acid derivative in presence of H_3PO_3/POCl_3. The procedure led to formation of two molecules of corresponding H-bisphosphonic acid which attached together via a phosphate bridge. The investigated compound exhibits activities (IC_(50) value) ranging from 14-23 μM (corresponding to human neuroblastoma SK-BE (2) and SK-NM-C cells).