SYNTHESIS AND CYTOTOXIC ACTIVITY OF AZA-MICHAEL REACTION PRODUCTS FROM ETHYL SORBATE AND HETEROCYCLIC AMINES

被引：3

作者：

Suslov, E. V. ^{[1
]}

Korchagina, D. V. ^{[1
]}

Pokrovskii, M. A. ^{[2
]}

Pokrovskii, A. G. ^{[2
]}

Volcho, K. P. ^{[1
,2
]}

Salakhutdinov, N. F. ^{[1
,2
]}

机构：

[1] Russian Acad Sci, Siberian Branch, NN Vorozhtsov Novosibirsk Inst Organ Chem, Novosibirsk 630090, Russia

[2] Novosibirsk State Univ, Novosibirsk 630090, Russia

来源：

CHEMISTRY OF NATURAL COMPOUNDS | 2015年 / 51卷 / 02期

关键词：

ethyl sorbate; aza-Michael reaction; cytotoxicity; heterocyclic amines; cancer; SORBIC ACID; HYDROAMINATION; DERIVATIVES;

D O I：

10.1007/s10600-015-1264-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The solvent-free reaction of ethyl sorbate and several heterocyclic amines at room temperature was shown to give aza-Michael 1,4-addition products. The newly formed double bond in the principal product had the E-configuration. It was found that the synthesized compounds exhibited cytotoxicity against cancer cell lines CEM-13, U-937, and MT-4. The piperazine derivative of ethyl sorbate exhibited the greatest activity against cancer cell line U-937, for which the concentration causing 50% death of the tumor cells (CTD50) was 10 mu g/mL.

引用

页码：296 / 301

页数：6

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