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N 4 -(2-Amino-4-fluorophenyl)- N 1 -(3-{2-[2-(3-{[2-(2,6-dioxo-3-piperidyl)-1,3-dioxoisoindolin-4-yl]amino}propoxy)ethoxy]ethoxy}propyl)terephthalamide

ORCID
0000-0001-6559-2527
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany
Abdelsalam, Mohamed;
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany
Zessin, Matthes;
ORCID
0000-0003-3876-2695
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany
Schmidt, Matthias;
Affiliation
Department of Enzymology, Institute of Biochemistry, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany
Schutkowski, Mike;
ORCID
0000-0002-5985-9261
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany
Sippl, Wolfgang

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 N 4 -(2-amino-4-fluorophenyl)- N 1 -(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 1 H-NMR, 13 C-NMR, IR and HRMS. The title compound was tested in vitro against human class-I HDACs isoforms and showed IC 50 = 3.4 µM against HDAC3; however, it did not show degradation for the targeted HDACs.

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