ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > Epigenetics > HDAC inhibitors > Belinostat (PXD101)
Belinostat (PXD101) Chemical Properties
- Density 1.427±0.06 g/cm3(Predicted)
- HS Code 29350090
Belinostat (PXD101) Usage And Synthesis
- DescriptionBelinostat is a drug which was developed by Spectrum Pharmaceuticals and is currently marketed by Onxeo as Beleodaq®. The drug, which received fast track designation by the United States Food and Drug Administration (US FDA) and was approved for the treatment of hematological malignancies and solid tumors associated with peripheral T-cell lymphoma (PTCL) in 2014, is a histone deacetylase (HDAC) inhibitor and is the third such treatment to receive accelerated approval for PTCL, the others being vorinostat (Zolinza®) and pralatrexate (Folotyn®). Although belinostat was not yet approved in Europe as of August 2014, the compound exhibits a safety profile considered to be acceptable for HDAC inhibitors–less than 25% of patients reported adverse effects and these most frequently were nausea, fatigue, pyrexia, anemia, and emesis.
- UsesBelinostat is a novel histone deacetylase 3 selective inhibitor, which protects the β cells from cytokine-induced apoptosis.
- DefinitionChEBI: A hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity.
- Chemical SynthesisCommercially available 3-bromobenzenesulfonyl chloride (41)
was reacted with aniline in the presence of aqueous sodium carbonate
to deliver sulfonamide 42 in 94% yield. Next, this aryl bromide
was subjected to a Heck reaction involving ethyl acrylate to
give rise to cinnamate ester 43, which was immediately saponified
under basic conditions and acidic workup to furnish the corresponding
acid 44. This acid was activated as the corresponding acid
chloride prior to subjection to hydroxylamine under basic conditions
to form the hydroxamic acid, which was then recrystallized
from an 8:1 ethanol/water mixture in the presence of a catalytic
amount of sodium bicarbonate to furnish crystalline belinostat
(VI) in 87% overall yield from acid 44.
- N-[(2,3-dimethoxyphenyl)methyl]-3,4-dimethoxy-benzeneethanamine hydrochloride 2-Propenoic acid, 3-[3-[(phenylaMino)sulfonyl]phenyl]-, ethyl ester, (2E)- PXD-101 1,4-Bis[(4-chlorophenyl)-phenylMethyl]piperazine Panobinostat JNJ-26481585 Mocetinostat (MGCD0103) Vorinostat Entinostat CRA-02478 cinnamoylhydroxamic acid Belinostat (PXD101)
- Company Name:Dalian Wondersun Biochemical Technology Co., Ltd. Gold
- Company Name:Shanghai Boyle Chemical Co., Ltd.
- Company Name:J & K SCIENTIFIC LTD.
- Tel:400-666-7788 010-82848833-
- Company Name:Chembest Research Laboratories Limited
- Company Name:Jinan Trio PharmaTech Co., Ltd.
- Tel:+86 (531) 88811783
- Email:email@example.com (International market);firstname.lastname@example.org(Domestic market)
- Oct 21，2019