INVESTIGADORES
RADIVOY gabriel Eduardo
artículos
Título:
Novel Alkynylphosphonate Analogue of Calcitriol with Potent Antiproliferative Effects in Cancer Cells and Lack of Calcemic Activity
Autor/es:
D. SALOMÓN; S. GRIOLI; M. BUSCHIAZZO; E. MASCARÓ; C. VITALE; G. RADIVOY; M. PEREZ; Y. FALL; E. MESRI; A. CURINO; M. FACCHINETTI
Revista:
ACS MEDICINAL CHEMISTRY LETTERS
Editorial:
AMERICAN CHEMICAL SOCIETY
Referencias:
Año: 2011 vol. 2 p. 503 - 508
ISSN:
1948-5875
Resumen:
Here, we describe the design and synthesis of diethyl [(5Z,7E)-(1S,3R)- 1,3-dihydroxy-9,10-secochola-5,7,10(19)-trien-23-in-24-yl] phosphonate (compound 10), which combines the low calcemic properties of phosphonates with the decreased metabolic inactivation due to the presence of a triple bond in C-24 and studied its in vitro effects on several cancer cell lines and its in vivo effects on blood calcium levels. We demonstrate that this compound is a potent antiproliferative vitamin D analogue, showing lack of calcemic effects in vivo.