Work

Design, synthesis, and evaluation of novel hydrazide and hydroxamate derivatives as potent antileukemic agents with preferential HDAC-2 inhibitory activity over class I isoform

Year: 2026

Type: article

Abstract: of 5.23 µM. Western blot analyses in SEM cells revealed that the lead compound 7a bound to its intracellular target, resulting in an approximately 59% reduction in total HDAC-2 protein levels. Flow cytometry revealed that a significant reduction in HDAC-2 led to cancer cells being arrested at the key G2/M phase of the cell cycle, with 46.22% of cells detained there compared to merely 7.21% in untreated controls. Subsequent analysis using Annexin V/PI labeling demonstrated that this cell cycle arrest results in a significant elevation of programmed cell death, increasing total apoptosis to 31.12%, while maintaining non-specific necrosis at a minimal 4.29%. Taken together, these findings indicate that the 4-iodo-3-nitrophenyl compounds are effective tools for the targeted treatment of leukemia, displaying preferential HDAC-2 inhibitory activity among the evaluated class I isoforms.

Source: RSC Advances

DOI: 10.1039/d6ra08049a

Authors: Fatma Elzahraa Ali, Abdullah Yahya Abdullah Alzahrani, Bandar A. Alyami, Stefan Bräse, Anber F. Mohammed, Bahaa G. M. Youssif

Institutions: Assiut University, King Khalid University, Najran University, Karlsruhe Institute of Technology

Language: English

Topic: Histone Deacetylase Inhibitors Research

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $1,042