Please use this identifier to cite or link to this item:
http://dx.doi.org/10.25673/101459
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, Matthias ![]() Schutkowski, Mike Sippl, Wolfgang ![]() |
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. |
URI: | https://opendata.uni-halle.de//handle/1981185920/103417 http://dx.doi.org/10.25673/101459 |
Open Access: | ![]() |
License: | ![]() |
Journal Title: | Molbank |
Publisher: | MDPI |
Publisher Place: | Basel |
Volume: | 4 |
Original Publication: | 10.3390/M1501 |
Appears in Collections: | Open Access Publikationen der MLU |
Files in This Item:
File | Description | Size | Format | |
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molbank-2022-M1501.pdf | 1.41 MB | Adobe PDF | ![]() View/Open |