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Information × Registration Number 0223U000280, 0120U100309 , R & D reports Title Directed synthesis of novel nitrogen- and oxygencontaining heterocyclic compounds as low molecular weight bioregulators. popup.stage_title Head Brovarets Volodymyr S., Доктор хімічних наук Registration Date 05-01-2023 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2 An approach to the synthesis of new 5-amino-4-cyanoxazoles with a carboxyl group in the C-2 position, connected to the heterocycle directly or through an aliphatic linker, was described. The process is characterized by readily available raw materials, ease of operation and high product yield. Wide applicability of the synthesized compounds in organic synthesis was also successfully demonstrated. The problem of developing new antiviral drugs against human cytomegalovirus (HCMV) using chemical modeling (OCHEM) was studied. Six most promising imidazole derivatives were identified and synthesized and their antiviral activity against HCMV was investigated in vitro. The anticancer activity of a series of 3-(hetaryl/aryl)aminosubstituted isoquinolin-1(2H)-ones was studied as part of the international scientific program «NCI-60 Human Tumor Cell Lines Screen». The most effective compounds were those with thiazolyl or pyrazolyl substituent at 3-amino group of the isoquinoline cycle. We identified a new lead compound, 3-(1,3-thiazol-2-ylamino)isoquinolin-1(2H)-one, which effectively prevents tumor cell growth (average lg GI50 = -5.18, lg TGI = -4.1, lg LC50 > -4.0) with good selectivity. A series of difunctionally substituted 1,2-dihydrophthalazines was obtained and their anticancer activity was investigated. The most effective compounds were those with an aryl substituent at N-2 of the phthalazine cycle: 4-(4-chlorophenyl)-2-(4-methylphenyl)-1,2-dihydrophthalazine (average lg GI50 = -5.79, lg TGI = -5.42, lg LC50 = -4.97) and 2,4-bis-(4-chlorophenyl)-1,2-dihydrophthalazine (average lg GI50 = -5.57, lg TGI = -5.08, lg LC50 = -4.61). Product Description popup.authors Ivanova Irina V. Bagreeva Oksana S. Brusnakov Mykhailo Yu. Velihina Yeheniia S. Vydzhak Roman M. Herasymov Yehor S. Golovchenko Оleksandr V. Didiv Nataliya D. Demydchuk Bogdan A. Zhirnov Viktor V. Zyabrev Volodymyr S. Kachaeva Maryna V. Kachkovskyi Oleksiy D. Кlyuchko Svitlana V. Kozachenko Olexandr P. Kondratyuk Kostyantyn M. Konovalenko Artem S. Los Oleksandr V. Mityukhin Оleg P. Merzhievskiy Danylo O. Moskvina Viktoria S. Mrug Galyna P. Pilyo Stepan G. Panchyshyn Svitlana Ya. Porhun Svitlana V. Potikha Lyudmyla M. Prokopenko Volodumir M. Prostota Yaroslav O Rentsevych Тetiana L. Severin Oleksandr O. Synenko Vitaliy O. Slyvchuk Serhiy R. Solomyanyi Roman M. Fedorenko Оlena А. Frasinyuk Mykhaylo S Tsygankova Vyktorya A. Charochkina Larysa L. Chumachenko Svitlana A. Shablykin Оleg V. Shablykina Olga V. popup.nrat_date 2023-01-05 Close