新型泊马度胺二苯脲衍生物的设计、合成及生物活性研究

IF 1.3 3区化学 Q3 CHEMISTRY, ORGANIC

Heterocyclic Communications Pub Date : 2022-01-01 DOI:10.1515/hc-2022-0155

Bin Sun, Xiaofei Liu, Tao Ji, Xiaoguang Zhan, L. Mao, Peng Deng, Lin Shi

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引用次数: 0

摘要

摘要以2-(2,6-二氧哌替啶-3-酰基)-4-氟异吲哚-1,3-二酮为原料，通过取代反应、点击反应和加成反应合成了一系列新型泊马度胺-二苯脲衍生物。这些化合物的结构经1H NMR、13C NMR和ms证实。我们在体外实验中发现，部分化合物能够抑制吲哚胺吡罗-2,3-双加氧酶-1的活性，其中5b的抑制活性达到了有益的水平。图形抽象

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Design, synthesis, and biological activity of novel pomalidomide linked with diphenylcarbamide derivatives

Abstract Based on 2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione as a raw material, a series of novel pomalidomide linked with diphenylcarbamide derivatives were synthesized through several step reactions of substitution, click reaction, and addition reaction. The structures of these compounds were confirmed by 1H NMR, 13C NMR, and MS. We discovered that some of the compounds are capable of suppressing indoleamine pyrrole-2,3-dioxygenase-1 activities in in vitro experiments, in which the inhibitory activity of 5b reached the level of benefits. Graphical abstract

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来源期刊

Heterocyclic Communications 化学-有机化学

CiteScore

3.80

自引率

4.30%

发文量

审稿时长

1.4 months

期刊介绍： Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.