期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 2, 期 7, 页码 503-508出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml200034w
关键词
1 alpha,25-(OH)(2) vitamin D(3); alkynylphosphonate analogues; cancer; hypercalcemia; cellular proliferation
资金
- National Council of Scientific and Technical Research (CONICET)
- National Agency for Scientific and Technological Promotion (ANPCyT)
- Universidad Nacional del Sur (SGCyT-UNS), Argentina
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.
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