HETEROCYCLIC COMPOUNDS, HAVING ANTIPROLIFERATIVE ACTIVITY AND METHOD OF SLOWING DOWN TUMOUR CELL PROLIFERATION Russian patent published in 2011 - IPC C07D239/54 A61P35/00 

Abstract RU 2429232 C2

FIELD: chemistry.

SUBSTANCE: agent is derivatives of bis(5-methylaminomethyluracil)polymethylene of formula (I) or pharmaceutically acceptable salts thereof

.

The agent is specifically a compound selected from: 5-[4-(2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidinylmethylamino)propylaminomethyl]-1,2,3,4-tetrahydro-2,4-pyrimidine dione (n=1); 5-[4-(2,4-dioxo-1,2,3,4-tetrahydro-5- pyrimidinylmethylamino)butylaminomethyl]-1,2,3,4-tetrahydro-2,4-pyrimidine dione (n=2);5-[4-(2,4-dioxo-1,2,3,4-tetrahydro-5- pyrimidinylmethylamino)pentylaminomethyl]-1,2,3,4-tetrahydro-2,4-pyrimidine dione (n=3) and 5-[4-(2,4-dioxo-1,2,3,4-tetrahydro-5- pyrimidinylmethylamino)hexylaminomethyl]-1,2,3,4-tetrahydro-2,4- pyrimidine dione (n=4). The disclosed compound was found to have in vitro capacity to increase activity of di- and polyamine oxidase, reduce ornithine decarboxylase activity, particularly in tumour cells, specifically tumour cells of human ovarian carcinoma. The disclosed compounds have in vitro low cytotoxicity. The invention also relates to a method of slowing down tumour cell proliferation using compounds of formula (1).

EFFECT: improved properties of inhibitor of formation of polyamines, low rate of tumour cells proliferation.

6 cl, 4 dwg, 11 tbl, 4 dwg

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RU 2 429 232 C2

Authors

Shevchenko Anna Aleksandrovna

Sjatkin Sergej Pavlovich

Levov Aleksandr Nikolaevich

Beninati Simone

Fedoronchuk Tamara Vasil'Evna

Dates

2011-09-20Published

2008-12-29Filed