Konovalenko A. Konovalenko A. S. 3-Acyl(aza)isochromones in the synthesis of new bioactive hetaryl substituted and hetero-fused azines

Українська версія

Thesis for the degree of Doctor of Philosophy (PhD)

State registration number

0823U101533

Thesis Registration Form

0823U101533.pdf

Applicant for

Specialization

  • 102 - Хімія

12-12-2023

Specialized Academic Board

Наказ № 2680

V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine

Essay

The qualifying work is devoted to the development of effective and convenient methods for the preparative synthesis of new 3-hetarylsubstituted and hetero-fused isoquinoline derivatives, as well as hetaryl-substituted naphthyridines, based on available multifunctional reagents: 3-acyl(aza)isochromones (3 acyl(aza)-isocoumarins). 8-Amino-6-(2 R-thiazol-4 yl)-1,7-naphthyridines, as well as parent 1-amino-3 hetaryl-isoquinolines, and unlike their precursors, due to the presence of aliphatic amine residue have high solubility in organic solvents (EtOAc, toluene) and in weakly acidic aqueous solutions, which will be favorable for further biological tests. The high anticancer activity predicted for certain types of synthesized substances has been confirmed by appropriate tests.

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Research papers

1. Коноваленко, А. С.; Шабликін, О. В.; Шабликіна, О. В.; Москвіна, В. С.; Броварець, В. C.; Хиля, В. П. Оцінка протиракової активності похідних ізохіноліну – продуктів рециклізації 3-(2-(тієн-2-іл)тіазол-4-іл)ізокумарину. Доп. Нац. акад. наук Укр. 2019, (12), 83–90

2. Konovalenko, A. S.; Shablykin, O. V.; Brovarets, V. S., Shablykina, O. V.; Moskvina, V. S.; Kozytskiy, A. V. 3-Hetarylisocoumarins in the synthesis of 1 functionalized 3-hetarylisoquinolines. Chem. Heterocycl. Comp. 2020, 56 (1), 1021–1029

3. Konovalenko, A. S.; Zhirnov, V. V.; Shablykin O. V.; Shablykina O. V.; Moskvina V. S.; Brovarets V. S. The effect of heterocyclic substituent at C-3 position of 1-(4-methyl-piperazin-1-yl) isoquinolines on their anticancer activity. Biopolymers and Cell 2022, 38 (1), 37–47

4. Konovalenko, A. S.; Shablykina, O. V.; Shablykin, O. V.; Moskvina, V. S.; Brovarets, V. S. 1H-isochromene-1-ones and isoquinoline-1(2H)-ones with carbonyl group in position 3: Features of synthetic approaches and transformation. Arkivoc 2022, Part (viii), 79–112

5. Коноваленко, А. С.; Шабликін, О. В.; Шабликіна, О. В.; Броварець, В. C.; Хиля, В. П. Простий підхід до створення системи 1,3,4,6,11,11a-гексагідро-2H-піразино[1,2-b]ізохіноліну. Доп. Нац. акад. наук Укр. 2023, (4), 43–51

6. Konovalenko, A. S.; Shablykin, O. V.; Shablykina, O. V.; Moskvina, V. S.; Shishkina, S. V.; Kozytskiy, A. V.; Brovarets, V. S. Distinctive features of 3 acetyl- and 3-benzoyl-isocoumarins' interaction with active primary amines. ChemistrySelect 2023, 8 (37), e202301380.

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Files

Dis-Коноваленко.doc

autoreferat-АНОТАЦІЯ.docx

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