Synthesis of Selagibenzophenone A and Its Derivatives for Evaluation of Their Antiproliferative, RORγ Inverse Agonistic, and Antimicrobial Effect **
Abstract: We report a modular synthetic approach towards novel derivatives of the naturally occurring arylated benzophenone selagibenzophenone A. The initial strategy for the construction of the carbon framework of the derivatives relied on the Suzuki reaction of 2,4,6‐tribromobenzonitrile, and the addition of the aryl lithium species to nitrile to generate imine. However, the formed imines showed remarkable stability toward hydrolysis. Therefore, Suzuki cross‐coupling was carried out with 2,4,6‐tribromobenzaldehyde and the subsequent addition of organometallic species to the aldehyde. Oxidation of the resulting alcohol ensured the access to desired ketones. The importance of the developed modular strategy is underlined by the discovery of several derivatives with selective cytotoxic effects and potential anti‐inflammatory activity superior to the effect of the natural product.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Synthesis of Selagibenzophenone A and Its Derivatives for Evaluation of Their Antiproliferative, RORγ Inverse Agonistic, and Antimicrobial Effect ** ; volume:8 ; number:7 ; year:2023 ; extent:8
ChemistrySelect ; 8, Heft 7 (2023) (gesamt 8)
- Creator
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Lapinskaite, Ringaile
Atalay, Hazal Nazlıcan
Malatinec, Štefan
Donmez, Serhat
Cinar, Zeynep Ozlem
Schwarz, Patrik F.
Perhal, Alexander F.
Císařová, Ivana
Labanauskas, Linas
Karpiński, Tomasz M.
Dirsch, Verena
Tumer, Tugba Boyunegmez
Rycek, Lukas
- DOI
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10.1002/slct.202204816
- URN
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urn:nbn:de:101:1-2023021414194795652579
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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14.08.2025, 10:48 AM CEST
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Lapinskaite, Ringaile
- Atalay, Hazal Nazlıcan
- Malatinec, Štefan
- Donmez, Serhat
- Cinar, Zeynep Ozlem
- Schwarz, Patrik F.
- Perhal, Alexander F.
- Císařová, Ivana
- Labanauskas, Linas
- Karpiński, Tomasz M.
- Dirsch, Verena
- Tumer, Tugba Boyunegmez
- Rycek, Lukas