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Information × Registration Number 0224U031472, 0122U001809 , R & D reports Title Molecular design of bioisosters of natural compounds and multicomponent materials for targeted drug delivery popup.stage_title Head Volovenko Yulian М., Доктор хімічних наук Registration Date 01-05-2024 Organization Taras Shevchenko National University of Kyiv popup.description2  The literature on cyclic sulfinamides (put simply, sultims) published from 1989 to 2022 has been summarized and reviewed. The data presented will be useful to specialists in different areas, especially those who work in the field of synthetic organic and pharmaceutical chemistry. We describe the reaction of carbonitriles with α-functionalized sulfonyl chlorides and the reactivity of resulting α-functionalized β-enamino γ-sultams. The analysis of the results of a complex study involving physical methods (NMR and IR spectroscopy, X-ray diffraction study) and DFT calculations (performed at PBE0 QZVP level of theory) allowed us to rationalize and formulate the rules of structure‒activity relationship for the discussed sultams. We developed method for two-step synthesis of quite underrepresented heterofused esultams annelated on face [d]. Thus, alkyl 2-(methylsulfonamidomethyl)hetaryl carboxylates readily participate in the sulfa-Dieckmann condensation to give the desired heterofused e-sultams. The method showed a broad substrate scope while the target compounds demonstrated a great synthetic potential. We designed and synthesized a series of novel γ,γ-disubstituted β-keto ε-sultams, prepared a number of derivatives and evaluated their cytotoxic activity against MDA-MB-231 breast cancer cell line. This class of compounds can be considered as valuable building blocks since they possess carbonyl functionality and an EWG-activated methylene group capable of further functionalization. Despite the prepared β-keto ε-sultams showing weak cytotoxicity against the MDA-MB-231 breast cancer cell line, their pyrazolofused derivatives appeared perspective pharmacological templates with stable cytotoxic effects. Moreover, β-keto ε-sultams and their heterofused derivatives form watersoluble conjugates with branched polymers based on dextran-polyacrylamide (D-PAA) that can be used as the transport module for targeted drug delivery in biological media. Product Description popup.authors Virych Pavlo A. Vashchenko Bohdan V. Dobrydniev Oleksii V. Kuziv Yuliia I. Popova Mariia V. Chumachenko Vasyl A. popup.nrat_date 2024-05-01 Close