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Information × Registration Number 0224U032934, (0123U103123) , R & D reports Title Directed synthesis of new heterocyclic sulfonamides as potential anticancer agents popup.stage_title Нові сульфоніламіди бісоксазолів та 4-фосфорильованих похідних оксазолу: синтез, характеристика, in silico та in vitro дослідження протиракової активності. Head Kachaieva Maryna V., к.х.н. Registration Date 11-12-2024 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description1 Synthesis of new bioactive sulfamides of the oxazole series with antitumor activity. The work plans the use and development of convenient synthetic methods for obtaining new oxazoles and bisoxazoles, the use of in silico modeling to predict the anticancer activity of oxazole derivatives, the assessment of antitumor activity and the study of the interdependence of the activity of synthesized substances from the structure. popup.description2 According to the results of QSAR prediction, fourteen new N-(4-cyano-1,3-oxazol-5-yl)sulfonamides were synthesized, among which 2 compounds (N-(4-cyano-2-phenyl-1,3-oxazol-5-yl)-N,4-dimethyl-benzenesulfonamide and N-(4-cyano-2-(thiophen-2-yl)-1,3-oxazol-5-yl)-N,4-dimethylbenzenesulfonamide) showed anticancer activity within the GI50 parameter. Disruption of microtubule formation may be one of the mechanisms of their anticancer action. Six compounds containing two 1,3-oxazole rings connected by a sulfonylpiperazine linker were obtained. 5-((4-(4-Cyano-2-(p-tolyl)-1,3-oxazol-5-yl)piperazin-1-yl)sulfonyl)-2-(p-tolyl)-1,3-oxazole-4-carbonitrile showed anticancer activity and selectivity against leukemia lines. Seven new representatives of 5-sulfanyl-substituted (thiazol-4-yl)phosphonium salts were synthesized and tested for their anticancer activity in vitro in a one-dose and five-dose NCI-60 experiment. The overall average parameters were: GI50 = 0.3–2.7 μM, TGI = 7.0–14.6 μM and LC50 = 3.6–41.8 μM. Their mechanism of action may be related to DNA. The results of the work show that N-(4-cyano-1,3-oxazol-5-yl)sulfonamides, sulfonamide derivatives of bisoxazole, and 4-phosphorylated derivatives of 1,3-thiazole are valuable molecules for searching among them for bioactive compounds with anticancer activity characterized by selectivity towards individual cancer lines. Product Description popup.authors Bahrieieva Oksana S. Hodyna Diana M. Severin Oleksandr O. popup.nrat_date 2024-12-11 Close