SYNTHESIS AND BIOLOGICAL EVALUATION OF MC-1357, A NEW 20-EPI-23-OXA-1-ALPHA,25-DIHYDROXY-VITAMIN-D3 ANALOG WITH POTENT NONCLASSICAL EFFECTS

被引：15

作者：

CALVERLEY, MJ ^{[1
]}

BINDERUP, L ^{[1
]}

机构：

[1] LEO PHARMACEUT PROD,DEPT BIOL,DK-2750 BALLERUP,DENMARK

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)80117-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of the 20-epi-23-oxa-24a,24b-dihomo analogue (MC 1357) of 1alpha,25-dihydroxy-vitamin D3 is described. In classical receptor binding and in vivo calcemic effect assays MC 1357 is slightly less potent than the natural hormone. However, in its in vitro effects on cancer cell differentiation and proliferation and on the mixed lymphocyte reaction it is 2 to 3 orders of magnitude more potent.

引用

页码：1845 / 1848

页数：4

共 13 条

[1] 20-EPI-VITAMIN-D3 ANALOGS - A NOVEL CLASS OF POTENT REGULATORS OF CELL-GROWTH AND IMMUNE-RESPONSES [J].

BINDERUP, L ;

LATINI, S ;

BINDERUP, E ;

BRETTING, C ;

CALVERLEY, M ;

HANSEN, K .

BIOCHEMICAL PHARMACOLOGY, 1991, 42 (08) :1569-1575

[2]

BRETTING C, 1991, VITAMIN D, P159

[3]

Calverley M. J., 1992, ANTITUMOR STEROIDS, P193

[4] SYNTHESIS OF MC-903, A BIOLOGICALLY-ACTIVE VITAMIN-D METABOLITE ANALOG [J].

CALVERLEY, MJ .

TETRAHEDRON, 1987, 43 (20) :4609-4619

[5]

CALVERLEY MJ, 1991, VITAMIN D, P163

[6]

GIELEN JWJ, 1980, RECL TRAV CHIM PAY B, V99, P306

[7]

HANSEN K, 1991, VITAMIN D, P161

[8]

HESSE RH, 1983, Patent No. 78704

[9]

KUBODERA N, 1991, CHEM PHARM BULL, V39, P3221, DOI 10.1248/cpb.39.3221

[10]

MURAYAMA E, 1986, CHEM PHARM BULL, V34, P4410

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