Structure-Activity Relationship Study of an Alkynylphosphonate and a Vynilphosphonate Analogues of Calcitriol

SILVINA MARIELA GRIOLI; ELIANA NOELIA ALONSO; EVANGELINA MASCARÓ; SANTIAGO ARMANDO STABILE; MARIA JULIA FERRONATO; MARIO ALFREDO QUEVEDO; GABRIEL RADIVOY; MARIA MARTA FACCHINETTI; CRISTIAN ALEJANDRO VITALE; ALEJANDRO CARLOS CURINO

MEDICINAL CHEMISTRY

BENTHAM SCIENCE PUBL LTD

Lugar: Oak Park; Año: 2020

1573-4064

1α,25-dihydroxyvitamin D3 (calcitriol) shows potent growth-inhibitory properties on different cancer cell lines but its hypercalcemic effects have severely hampered its therapeutic application. Therefore, it is important to develop synthetic calcitriol analogues that retain or even increase its antitumoral effects and lack hypercalcemic activity. Based on previous evidence of the potent antitumor effects of the synthetic alkynylphosphonate EM1 analogue, we have now synthesized a derivative called SG.