| Literature DB >> 15109656 |
Yuko Kato1, Yusuke Nakano, Hiroko Sano, Aya Tanatani, Hisayoshi Kobayashi, Rumiko Shimazawa, Hiroyuki Koshino, Yuichi Hashimoto, Kazuo Nagasawa.
Abstract
Novel vitamin D(3) analogs having a lactam structure in their side chains, 1 alpha,25-dihydroxyvitamin D(3)-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 1 alpha,25-dihydroxyvitamin D(3).Entities:
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Year: 2004 PMID： 15109656 DOI： 10.1016/j.bmcl.2004.02.076
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823