Structure-activity relationship of novel menaquinone-4 analogues : Modification of the side chain affects their biological activities
Structure-activity relationship of novel menaquinone-4 analogues : Modification of the side chain affects their biological activities
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新型menaquinone-4类似物的构效关系：侧链的修饰影响其生物活性
DOI：
10.1021/jm2013166
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
T
中科院分区：
文献类型：
--
作者：
Suhara;Y.; Hanada;N.; Okitsu;T.; Sakai;M.; Watanabe;M.; Nakagawa;K.; Wada;A.; Takeda;K.; Takahashi;K.; Tokiwa;H.; Okano;T
我们合成了新的维生素 K 类似物，其去甲基化或还原了 menaquinone-4 (MK-4) 侧链双键，并评估了它们的 SXR 介导的转录活性以及它们转化为 MK-4 的程度。结果表明，侧链部分7'位点甲基缺失的类似物影响了向MK-4的转化活性。相反，侧链部分双键数量的减少似乎降低了SXR介导的转录活性。
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′ 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.