Histone deacetylases (HDAC) represent promising epigenetic targets for several diseases including different cancer types. The HDAC inhibitors approved to date are pan-HDAC and most show a poor selectivity profile, side effects, in particular hydroxamic-acid-based lack good pharmacokinetic profiles. Therefore, the development of isoform-selective non-hydroxamic acid is highly regarded field medi...

Title:Suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses vasculogenic mimicry and proliferation of highly aggressive pancreatic cancer PaTu8988 cells

Histone deacetylase inhibitors (HDACi) target abnormal epigenetic states associated with a variety of pathologies, including cancer. Here, the development of a prodrug of the canonical broad-spectrum HDACi suberoylanilide hydroxamic acid (SAHA) is described. Although hydroxamic acids are utilized universally in the development of metalloenzyme inhibitors, they are considered to be poor pharmaco...

A series of few triazole linked hydroxamic acid derivatives were designed virtually considering the basic pharmacophore of suberoyl anilide hydroxamic acid (SAHA). The least energy conformers of each molecule was generated and docked with human histone deacetylase (HDAC8) with PDB id 1T69 using Autodock 4.0.1. Most of the molecules have shown significant binding interaction with the receptor. A...

OF ORGANOGERMANIUM AND ORGANOTIN DERIVATIVES OF HYDROXAMIC ACIDS Valery S. Petrosyan*, Natalia S. Yashina, and Sergei V. Ponomarev Department of Chemistry, M. V. Lomonosov University, Moscow 119899, Russia Hydroxamic acids as the precursors oftheir organogermanium and organotin derivatives have been themselves intensively studied fi’om the viewpoint of their potential biological activities [1-3...

Hydroxamic acids, R-CONHOH, are inhibitors specific to the respiratory pathway through the alternate, cyanide-insensitive terminal oxidase of plant mitochondria. The nature of the R group in these compounds affects the concentration at which the hydroxamic acids are effective, but it appears that all hydroxamic acids inhibit if high enough concentrations are used. The benzhydroxamic acids are e...

The zinc-metalloenzyme GlcNAc-PI de-N-acetylase is essential for the biosynthesis of mature GPI anchors and has been genetically validated in the bloodstream form of Trypanosoma brucei, which causes African sleeping sickness. We screened a focused library of zinc-binding fragments and identified salicylic hydroxamic acid as a GlcNAc-PI de-N-acetylase inhibitor with high ligand efficiency. This ...

The self-prepared pectin hydroxamic acid has been reported to have antioxidant activities [Yang, S. S., Cheng, K. D., Lin, Y. S., Liu, Y. W., & Hou, W. C. (2004). Pectin hydroxamic acids exhibit antioxidant activities in vitro. Journal of Agricultural and Food Chemistry, 52, 4270-4273]. In this study, the galacturonic acid (GalA), the monomer unit of the pectin polymer, was esterified with acid...

Disruption of glycosylphosphatidylinositol biosynthesis is genetically and chemically validated as a drug target against the protozoan parasite Trypanosoma brucei, the causative agent of African sleeping sickness. The N-acetylglucosamine-phosphatidylinositol de-N-acetylase (deNAc) is a zinc metalloenzyme responsible for the second step of glycosylphosphatidylinositol biosynthesis. We recently r...