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HDAC performs the reverse process of histone acetyl co A to the lysines on the histone, inducing a state known as hyper acetylation. Hyper acetylation causes a decreased binding of the histones to DNA and leads to chromatin expansion, allowing transcription to take place. Keywords: Keyword Histone deacetylase inhibitors, Matrix metalloproteinase inhibitors, HIV, Hydroxamaates, Ribonucleoside diphosphate reductase Cite this paper: David I. The reasonable way of producing hydroxamic acid derivative is the reaction of hydroxylamine with acid chlorides or esters. 13 Hydroxamic acids are capable of inhibiting a variety of enzymes, including ureases, 14, 15 peroxidises 16, and matrix metalloproteinases. Ugwu, Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria. Abstract Hydroxamates are physiologically active compounds. They have found applications as histone deacetylase inhibitors widely applied in cancer treatment such as vorinostat, belinostat, panobinostat and trichostatin A. They are amides where the hydrogen H atom of NH center has been replaced by an OH. Hydroxamates are deprotonated product of hydroxamic acid and acts as excellent ligand. Ugwuja3 1Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria 2National Centre for Energy Research and Development, University of Nigeria, Nsukka, Nigeria 3Department of Chemical Sciences, Federal University, Wukari, Nigeria Correspondence to: David I. Introduction Hydroxamates are class of organic compounds bearing the functional group RICON OH RII as organic residues and CO as a carbonyl group. Hyper acetylation of histones increases the access of some transcription factors to nucleosomes thereby increasing RNA transcription.
34 Application of ultra-sonication was showed to accelerate this conversion.
White et al 38 reported the synthesis of hydroxamates using Deoxo-fluor; Katritzky et al 39 reported the synthesis of N-alkyl, O-alkyl and O, N-dialkyl hydroxamic acids via acyl benzotriazole intermediates; Gissot et al 40 reported high yielding one step synthesis of hydoxamates from various un-activated esters including enolizable esters and chrial α-amino acid esters and peptides ; Woo et al 41 reported the conversion of sterically hindered carboxylic acids to N-methoxy-N-methyl amides using 1.1eq of methanesulphonyl chloride; Martinelli et al 42 reported the palladium catalysed amino carbonylation of anyl bromides into the corresponding Weinreb amides; Nemoto et al 43 also reported a one pot synthesis of α-siloxy weinreb amides from aldelydes using N, O-dimethly amine and a masked acyl cyamide reagent bearing a tert-butyl dimethyl silyl group. Synthesis of Anticancer Hydroxamates Most hydroxamates used in cancer chemotherapy acts as histone deacetylase HDAC inhibitors.
Histone deacetylase are a group of enzymes that removes acetyl groups from the lysine residues on a histone.
Carbodiimides hydrolyze to form ureas, which makes them uncommon in nature. Hydroxyurea are also used for treatment of chronic myelogenal leukemia, myeloproliferative syndromes and sickle cell anemia. 2 Hydroxamates of amino acids are effective inhibitors of amino peptidases.
From the perspective of small molecule activation, carbodiimides are. Hydroxamates such as fosmidomycin and desferrioxamine B are potent antimalarial agent. Ugwuja, Synthesis and Biological Applications of Hydroxamates, American Journal of Organic Chemistry, Vol. 3 Their mode of action results from the formation of bidentate ligand with active site of zinc.