sp2桥连二芳基类视黄醇：桥连区域取代对视黄醇X受体（RXR）选择性的影响
sp2-bridged diaryl retinoids: effects of bridge-region substitution on retinoid X receptor (RXR) selectivity.
作者信息
Dawson M I, Hobbs P D, Jong L, Xiao D, Chao W R, Pan C, Zhang X K
机构信息
Medicinal Chemistry Department, Molecular Medicine Research Institute, Mountain View, CA 94043, USA.
出版信息
Bioorg Med Chem Lett. 2000 Jun 19;10(12):1307-10. doi: 10.1016/s0960-894x(00)00243-2.
Abstract
RXR class selectivity and RXR transcriptional activation activity compared to those for the retinoic acid receptor subtypes were enhanced on the 4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenylethenyl)be nzoic acid scaffold and its 3-methyl analogue by replacing their 1,1-ethenyl bridge by a 1,1-(2-methylpropenyl) or cyclopropylidenylmethylene group.
摘要
与视黄酸受体亚型相比，通过将4-(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘乙烯基)苯甲酸支架及其3-甲基类似物的1,1-乙烯基桥替换为1,1-(2-甲基丙烯基)或环亚丙基亚甲基，RXR类选择性和RXR转录激活活性得到了增强。
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