New potent N‐hydroxycinnamamide‐based histone deacetylase inhibitors suppress proliferation and trigger apoptosis in THP‐1 leukaemia cells

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14160%2F25%3A00141158" target="_blank" >RIV/00216224:14160/25:00141158 - isvavai.cz</a>

Result on the web

<a href="https://onlinelibrary.wiley.com/doi/10.1002/ardp.202400889" target="_blank" >https://onlinelibrary.wiley.com/doi/10.1002/ardp.202400889</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1002/ardp.202400889" target="_blank" >10.1002/ardp.202400889</a>

Result language

angličtina

Original language name

New potent N‐hydroxycinnamamide‐based histone deacetylase inhibitors suppress proliferation and trigger apoptosis in THP‐1 leukaemia cells

Original language description

A new group of potent histone deacetylase inhibitors (HDACis) capable of inhibiting cell growth and affecting cell-cycle progression in Tohoku Hospital Pediatrics-1 (THP-1) monocytic leukaemia cells was synthesized. The inhibitors belong to a series of hydroxamic acid derivatives. We designed and synthesized a series of 22 N-hydroxycinnamamide derivatives, out of which 20 are new compounds. These compounds contain various substituted anilides as the surface recognition moiety (SRM), a p-hydroxycinnamate linker, and hydroxamic acids as the zinc-binding group (ZBG). The whole series of synthesized hydroxamic acids inhibited THP-1 cell proliferation. Compounds 7d and 7p, which belong to the category of derivatives with the most potent antiproliferative properties, exert a similar effect on cell-cycle progression as vorinostat and induce apoptosis in THP-1 cells. Furthermore, compounds 7d and 7p were demonstrated to inhibit HDAC class I and II in THP-1 cells with comparable potency to vorinostat and increase acetylation of histones H2a, H2b, H3, and H4. Molecular modelling was used to predict the probable binding mode of the studied HDACis in class I and II histone deacetylases in terms of Zn2+ ion chelation by the hydroxamate group.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

30104 - Pharmacology and pharmacy

Project

—

Continuities

—

Publication year

2025

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Archiv der Pharmazie

ISSN

0365-6233

e-ISSN

1521-4184

Volume of the periodical

358

Issue of the periodical within the volume

4

Country of publishing house

DE - GERMANY

Number of pages

22

Pages from-to

1-22

UT code for WoS article

001456667500001

EID of the result in the Scopus database

2-s2.0-105002082514