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Abdelsalam, M.* ; Ibrahim, H.S.* ; Krauss, L.* ; Zessin, M.* ; Vecchio, A.* ; Hastreiter, S. ; Schutkowski, M.* ; Schneider, G.* ; Sippl, W.*

Development of pyrazine-anilinobenzamides as histone deacetylase HDAC1-3 selective inhibitors and biological testing against pancreas cancer cell lines.

Methods Mol. Biol. 2589, 145-155 (2023)
DOI PMC
Open Access Green möglich sobald Postprint bei der ZB eingereicht worden ist.
Class I histone deacetylase (HDAC) enzymes are key regulators of cell proliferation and are frequently dysregulated in cancer cells. Here we describe the synthesis of a novel series of class-I selective HDAC inhibitors containing anilinobenzamide moieties as ZBG connected with a central (piperazin-1-yl)pyrazine moiety. Compounds were tested in vitro against class-I HDAC1, 2, and 3 isoforms. Some highly potent HDAC inhibitors were obtained and were tested in pancreatic cancer cells and showed promising activity. Moreover, we summarize how the growth-inhibitory effects of these compounds can be determined in murine pancreatic cancer cell lines.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Korrespondenzautor
Schlagwörter Anilinobenzamides ; Capping Group ; Class-i Histone Deacetylases Inhibitors ; Hdac ; Pancreas Cancer
ISSN (print) / ISBN 1064-3745
e-ISSN 1940-6029
Bandtitel HDAC/HAT Function Assessment and Inhibitor Development
Quellenangaben Band: 2589, Heft: , Seiten: 145-155 Artikelnummer: , Supplement: ,
Verlag Springer
Verlagsort Berlin [u.a.]
Nichtpatentliteratur Publikationen
Begutachtungsstatus Peer reviewed