支链色胺作为调节其抗增殖活性的一种工具。
Branching tryptamines as a tool to tune their antiproliferative activity.
作者信息
Salikov Rinat F, Trainov Konstantin P, Belousova Irina K, Belyy Aleksandr Yu, Fatkullina Ulyana Sh, Mulyukova Regina V, Zainullina Liana F, Vakhitova Yulia V, Tomilov Yury V
机构信息
N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky Prospect, 119991 Moscow, Russian Federation.
Moscow Chemical Lyceum, 4 Tamozhennyj Proezd, 111033 Moscow, Russian Federation.
出版信息
Eur J Med Chem. 2018 Jan 20;144:211-217. doi: 10.1016/j.ejmech.2017.12.028. Epub 2017 Dec 9.
The influence of a series of tryptamine derivatives on the viability of normal (HEK293) and tumor (HepG2, Jurkat and SH-SY5Y) cells has been evaluated. All tryptamines tested were three different substitution types: C- and N-branching, and indole benzylation. All the derivations enhance the activity of compounds separately, although the effects of different substitutions were not additive. Thus, combinations of C- and N-branchings as well as C-branching and indole benzylation gave little or no increase in activity.
已评估了一系列色胺衍生物对正常（HEK293）和肿瘤（HepG2、Jurkat和SH-SY5Y）细胞活力的影响。所测试的所有色胺均为三种不同的取代类型：C-和N-支链，以及吲哚苄基化。所有衍生物均分别增强了化合物的活性，尽管不同取代的效果并非相加性的。因此，C-和N-支链以及C-支链与吲哚苄基化的组合在活性上几乎没有增加或没有增加。
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