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Наукові видання. (Клінічна фармація ФПО) >

Please use this identifier to cite or link to this item: http://dspace.zsmu.edu.ua/handle/123456789/15386

Название: Anti-tumor potential of substituted 6-oxo(thioxo)-6,7-dihydro-2H-[1,2,4]triazino[2,3-с]quinazolin-2-ones
Авторы: Berest, G. G.
Nosulenko, I. S.
Voskoboynik, O. Yu.
Kovalenko, S. I.
Берест, Галина Григорівна
Носуленко, Інна Степанівна
Воскобойнік, Олексій Юрійович
Коваленко, Сергій Іванович
Issue Date: 2021
Издатель: Sherman Oaks, Los Angeles : GS publishing service
Библиографическое описание: Anti-tumor potential of substituted 6-oxo(thioxo)-6,7-dihydro-2H-[1,2,4]triazino[2,3-с]quinazolin-2-ones / G. G. Berest, I. S. Nosulenko, O. Yu. Voskoboynik, S. I. Kovalenko ; сompiled by V. Shpak // Scientific research of the XXI century. Volume 1 : collective monograph. - Sherman Oaks, Los Angeles : GS publishing service, 2021. – P. 295-311. - https://doi.org/10.51587/9781-7364-13302-2021-001
Аннотация: Quinazoline moiety may be found in structure of drugs that reveal wide spectrum of biological activity1, including anti-tumor effect2. Some of the quinazoline derivatives, namely 4-R-phenylaminoquinazolines («Gefitinib», «Erlotinib», «Vandetanib», «Lapatinib» etc) are inhibitors of CDK2 and p38 kinases, epidermal growth factor receptor, vascular endothelial growth factor and currently used in clinical oncology3. It should be mentioned, that antitumor activity of 4-R-phenylaminoquinazolines caused is determined by as nature of basic heterocyclic fragment, so by structure of aniline fragment in position 4. The presence of halogen, hydroxy-group or cyano-group in aniline moiety is essential for the presence of anticancer activity as well. The introduction of additional functional groups to position 6 and 7 is also reasonable for improvement of pharmacokinetic properties, namely bioavailability and lipophilicity. Thus, introduction of vinyl, but-2-ynamide fragments to the molecule increase the metabolic and excretion rate and consequently decrease cumulation of compounds. At the same time presence of alkoxy-groups and saturated nitrogen-containing moities and oxygen containing heterocyclic fragments is essential for hydrophobic interaction with target enzyme4. Moreover, recently, it was shown that annulation of heterocyclic fragment to pyrimidine ring (bioisosteric substitution) resulted the extension of anti-cancer activity spectrum, increasing of anti-cancer activity and decreasing of the agent’s toxicity5.
Описание: Берест Г. І. - 0000-0001-6718-1713; Носуленко І. С. - 0000-0002-8725-7321; Воскобойнік О. Ю. - 0000-0002-5790-3564; Коваленко С. І. - 0000-0001-8017-9108
URI: http://dspace.zsmu.edu.ua/handle/123456789/15386
ISBN: 978-1-7364133-0-2
Appears in Collections:Наукові видання. (Органічна хімія)
Наукові видання. (Фармакогнозія)
Наукові видання. (Клінічна фармація ФПО)

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