SYNTHESIS AND CYTOTOXIC ACTIVITY OF CONJUGATES OF (-)-CYTISINE AND THERMOPSIN AMINE DERIVATIVES WITH 1,3-DIMETHYL-5-FORMYLURACIL

被引：8

作者：

Tsypysheva, I. P. ^{[1
]}

Petrova, P. R. ^{[1
]}

Koval'skaya, A., V ^{[1
]}

Lobov, A. N. ^{[1
]}

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

Zainullina, L. F. ^{[2
]}

Vinogradova, V., I ^{[3
]}

Vakhitov, V. A. ^{[2
]}

Vakhitova, Yu V. ^{[2
]}

Galin, F. Z. ^{[1
]}

机构：

[1] Russian Acad Sci, Ufa Fed Res Ctr, Ufa Inst Chem, 71 Prosp Oktyabrya, Ufa 450054, Russia

[2] Russian Acad Sci, Ufa Fed Res Ctr, Inst Biochem & Genet, Ufa, Russia

[3] Acad Sci Uzbek, S Yu Yunusov Inst Chem Plant Subst, Tashkent, Uzbekistan

来源：

CHEMISTRY OF NATURAL COMPOUNDS | 2018年 / 54卷 / 05期

关键词：

quinolizidine alkaloids; (-)-cytisine; thermopsin; 1,3-dimethyl-5-formyluracil; cytotoxic activity; HEK293; Jurkat; HepG2; SOPHORIDINE; CARCINOMA;

D O I：

10.1007/s10600-018-2517-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New conjugates of the quinolizidine alkaloids (-)-cytisine and thermopsin were synthesized by alkylating their 9-amino derivatives with 1,3-dimethyl-5-formyluracil. The cytotoxic properties of the synthesized conjugates against cell lines HEK293, HepG2, and Jurkat were studied. Screening identified the lead compound 5-{[(3-benzyl-8-oxo-1,3,4,5,6,8-hexahydro-2H-1,5-methanopyrido[1,2-a][1,5]diazocin-9-yl)amino]methyl}-1,3-dimethylpyrimidine-2,4-(1H,3H)-dione, which suppressed metabolic activity of lymphoblastic leukemia cells with inhibitory concentration (IC50) 20.6 +/- 2.1 mu M (IC50 of reference compound 5-fluorouracil was 18.5 +/- 3.3 mu M).

引用

页码：938 / 946

页数：9

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