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Title: N4-(2-Amino-4-fluorophenyl)-N1-(3-{2-[2-(3-[[2-(2,6-dioxo-3-piperidyl)-1,3-dioxoisoindolin-4-yl]amino]propoxy)ethoxy]ethoxy}propyl)terephthalamide
Author(s): Abdelsalam, Mohamed
Zessin, Matthes
Schmidt, MatthiasLook up in the Integrated Authority File of the German National Library
Schutkowski, Mike
Sippl, WolfgangLook up in the Integrated Authority File of the German National Library
Issue Date: 2022
Type: Article
Language: English
Abstract: The design of proteolysis targeting chimeras (PROTACs) has become a promising technology for modifying a protein of interest (POI) through protein degradation. Herein, we describe the synthetic pathway to develop N4-(2-amino-4-fluorophenyl)-N1-(3-{2-[2-(3-{[2-(2,6-dioxo-3-piperidyl)-1,3-dioxoisoindolin-4-yl]amino}propoxy)ethoxy]ethoxy}propyl)terephthalamide, which was designed to work as a selective degrader of histone deacetylase-3 (HDAC3). The newly synthesized compounds were characterized by 1H-NMR, 13C-NMR, IR and HRMS. The title compound was tested in vitro against human class-I HDACs isoforms and showed IC50 = 3.4 µM against HDAC3; however, it did not show degradation for the targeted HDACs.
Open Access: Open access publication
License: (CC BY 4.0) Creative Commons Attribution 4.0(CC BY 4.0) Creative Commons Attribution 4.0
Journal Title: Molbank
Publisher: MDPI
Publisher Place: Basel
Volume: 4
Original Publication: 10.3390/M1501
Appears in Collections:Open Access Publikationen der MLU

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