摘要
本文综述了在化学合成萜二聚体药理学的进展,从天然化合物。合成萜二聚体分为特定亚组的基础对主要三萜单体骨架结构。二聚体结构的合成萜类衍生物可通过C-3羟基或另一组得到的共价键,VI一个2原子或C-17羧基(主要酸酐、酰胺或酯)。一些三萜类化合物可以发生化学转换导致的环状二聚体或其他类型的二聚体的形成美国的大部分得到三萜二聚体已进行药理试验评价其生物学活性,主要病毒(HIV-1 RT、HCVpp、VSVpp、hiv-rt-c8166-ccr5),细胞毒性(对如388、MCF-7、一定的ncih460,km20l2、DU-145、Hep-G2、A549、BGC-823,PC-3),抗炎(iNOS、原264.7)和糖尿病(rmgpa抑制)。作者还报告了OF部分所获得的循环三萜二聚体认与阴离子形成的自组装结构。
关键词: 三萜类、三萜二聚体,二聚衍生物,合成二聚体、萜类、三萜类化合物的药理活性。
Current Medicinal Chemistry
Title:Advances in Chemistry and Pharmacology of Triterpenoid Synthetic Dimers
Volume: 24 Issue: 20
关键词: 三萜类、三萜二聚体,二聚衍生物,合成二聚体、萜类、三萜类化合物的药理活性。
摘要: This review focuses on advances in chemistry and pharmacology of synthetic triterpenoid dimers, obtained from natural compounds. Synthetic triterpenoid dimers are divided into specific subgroups based on the structure of main triterpenoid monomeric skeleton. Synthetic triterpenoid derivatives of dimeric structure can be obtained through the covalent linkage of the C-3 hydroxyl or another group, via the C-2 atom or the C-17 carboxyl group (mainly anhydrides, amides or esters). Some triterpenes can undergo chemical transformations leading to the formation of cyclic dimers or other types of dimers. Most of the obtained triterpenoid dimers have been subjected to pharmacological tests evaluating their biological activity, mainly antiviral (HIV-1 RT, HCVpp, VSVpp, HIV-RT-C8166-CCR5), cytotoxic (against e.g. 388, MCF-7, SF-268, NCIH460, KM20L2, DU-145, Hep-G2, A549, BGC-823, PC-3), anti-inflammatory (iNOS, RAW 264.7) and antidiabetic (RMGPa inhibition). The authors also reported the ability of some of the obtained cyclic triterpenoid dimers to recognize anions and to form self-assembled structures.
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Advances in Chemistry and Pharmacology of Triterpenoid Synthetic Dimers, Current Medicinal Chemistry 2017; 24 (20) . https://dx.doi.org/10.2174/0929867324666170202151625
DOI https://dx.doi.org/10.2174/0929867324666170202151625 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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