Structure鈥揂ctivity Relationship of Novel Menaquinone-4 Analogues: Modification of the Side Chain Affects their Biological Activities
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- 作者：Yoshitomo Suhara ; Norika Hanada ; Takashi Okitsu ; Miho Sakai ; Masato Watanabe ; Kimie Nakagawa ; Akimori Wada ; Kazuyoshi Takeda ; Kazuhiko Takahashi ; Hiroaki Tokiwa ; Toshio Okano
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：February 23, 2012
- 年：2012
- 卷：55
- 期：4
- 页码：1553-1558
- 全文大小：296K
- 年卷期：v.55,no.4(February 23, 2012)
- ISSN：1520-4804
文摘
We synthesized new vitamin K analogues with demethylation or reduction of the double bonds of the side chain of menaquinone-4 (MK-4) and evaluated their SXR-mediated transcriptional activity as well as the extent of their conversion to MK-4. The results indicated that the analogue with the methyl group deleted at the 7鈥?site of the side chain part affected conversion activity to MK-4. In contrast, a decrease in the number of the double bonds in the side chain moiety appeared to decrease the SXR-mediated transcriptional activity.