A-ring hydroxymethyl 19-nor analogs of the natural hormone 1α,25-dihydroxyvitamin D3:: synthesis and preliminary biological evaluation

被引：14

作者：

Hatcher, MA

Peleg, S

Dolan, P

Kensler, TW

Sarjeant, A

Posner, GH ^{[1
]}

机构：

[1] Johns Hopkins Univ, Dept Chem, Baltimore, MD 21218 USA

[2] Univ Texas, MD Anderson Canc Ctr, Dept Med Specialties, Houston, TX 77030 USA

[3] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Div Environm Hlth Sci, Baltimore, MD 21205 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 12期

关键词：

calcitriol; 19-Nor; hydroxymethyl A-ring; novel analogs;

D O I：

10.1016/j.bmc.2005.04.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series 5-8 of 1- and 3-CH2OH 19-nor analogs of the hormone calcitriol (1) has been prepared. Surprisingly, 19-nor 1 alpha-CH2OH analog 5a is more antiproliferative at 100 nM concentration than the corresponding regioisomeric analog 6a with the natural lot-OH group, and 1 alpha-CH2OH hybrid analog 7a is similar in antiproliferative potency to calcitriol (1) even at low nanomolar concentrations. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：3964 / 3976

页数：13

共 29 条

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