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Registration Number

0219U005013, 0116U006000 , R & D reports

Title

COMPARATIVE STUDY OF NEW DERIVATIVES OF CHINASOLINE AND ERROLOTINBUS FOR THE DEFINITION OF A COMPOUND-LEADER PROVISION FOR INTRODUCTION IN ONCOLOGICAL PRACTICE (final)

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Head

Sharykina Nadiya Ivanivna, Demchenko Anatoliy Michailowich,

Registration Date

11-04-2019

Organization

State Institution "Institute of Pharmacology and Toxicology of National Academy of Medical Sciences of Ukraine"

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A comparative study of 31 new derivatives of quinazoline and Erlotinib was conducted. As a leader compound was selected compound 3105 that is superior to Erlotinib with activity in the cell culture of non-small cell lung cancer in humans (A549), has an antimetastatic effect, is related to low-toxicity substances, which makes it resonable for further preclinical studies and possible introduction into cancer practice non-small cell lung cancer. The high antitumor activity of the known drug-derivative quinazoline, alfa1-adrenoblockator with hypotensive action of doxazosin on the line of non-small cell lung cancer of the human (A549) is shown, which causes of its further study in order to spread clinical indications. It has been noted that the main mechanism of action of compound 3105 is the blockade of the activity of the epidermal growth factor receptor (EGFR) by inhibiting the tyrosine receptor phosphorylation, which is coupled with an EGFR transactivation blocking under the influence of the GPCR receptors. It was confirmed reasonable finding targeted antitumor agenents among condensed nitrogen-containing heterocycles.

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Акімова Н.
Баглай О.
Бакал Л.
Бобкова Л.
Борець А.
Гладиш Ю.
Голубов М.
Дабіжа Н.
Делян Є.
Демченко С.
Дніпрова Т.
Зоценко Л.
Карацуба Т.
Колядич О.
Максюта С.
Матвієнко А.
Паршиков О.
Рогозін В.
Середенко О.
Старікова О.
Хавич О.
Червіовський Д.
Шелест Д.

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2020-04-02