维生素D3的新型炔基膦酸酯类似物，在癌细胞中具有强大的抗增殖作用且无血钙活性。
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
作者信息
Salomón Débora G, Grioli Silvina M, Buschiazzo Maximiliano, Mascaró Evangelina, Vitale Cristian, Radivoy Gabriel, Perez Manuel, Fall Yagamare, Mesri Enrique A, Curino Alejandro C, Facchinetti María M
机构信息
Laboratorio de Biología Básica del Cáncer, Instituto de Investigaciones Bioquímicas Bahía Blanca (INIBIBB), 8000 , Bahía Blanca, Argentina.
Departamento de Química, Instituto de Química del Sur (Inquisur-Conicet), Universidad Nacional del Sur , 8000 Bahía Blanca, Argentina.
出版信息
ACS Med Chem Lett. 2011 Apr 11;2(7):503-8. doi: 10.1021/ml200034w. eCollection 2011 Jul 14.
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.
在此，我们描述了[(5Z,7E)-(1S,3R)-1,3-二羟基-9,10-断胆甾-5,7,10(19)-三烯-23-炔-24-基]膦酸二乙酯（化合物10）的设计与合成，该化合物将膦酸盐的低血钙特性与因C-24位存在三键而导致的代谢失活降低相结合，并研究了其对几种癌细胞系的体外作用及其对血钙水平的体内作用。我们证明该化合物是一种有效的抗增殖维生素D类似物，在体内显示出无血钙作用。
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