Title of article
Synthesis of 1α,25-dihydroxyvitamin D3-26,23-lactams (DLAMs), a novel series of 1α,25-dihydroxyvitamin D3 antagonist
Author/Authors
Yuko Kato، نويسنده , , Yusuke Nakano، نويسنده , , Hiroko Sano، نويسنده , , Aya Tanatani، نويسنده , , Hisayoshi Kobayashi، نويسنده , , Rumiko Shimazawa، نويسنده , , Hiroyuki Koshino، نويسنده , , Yuichi Hashimoto، نويسنده , , Kazuo Nagasawa، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
2579
To page
2583
Abstract
Novel vitamin D3 analogs having a lactam structure in their side chains, 1α,25-dihydroxyvitamin D3-26,23-lactams (DLAMs), were designed based on the principle of regulation of the folding of helix-12 in the vitamin D nuclear receptor (VDR). The new analogs were synthesized via 1,3-dipolar cycloaddition reaction and subsequent reduction of the isoxazolidine as key steps. Among the analogs, (23S,25S)-DLAM-01 (4a) and (23S,25S)-DLAM-1P (5a) bind strongly to VDR. Moreover, these analogs were found to inhibit the differentiation of HL-60 cells induced by 1α,25-dihydroxyvitamin D3.
Keywords
e-mail: nagasawa@iam.u-tokyo.ac.jp , fax: +81-358418495 , Vitamin D , Antagonist , Lactam.* Corresponding author. Tel.: +81-358417848
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794442
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