2565-10-8

Upstream product

• 67-56-1 methanol 
• 17625-03-5 m-sulfobenzoic acid, monosodium salt 

Downstream Products

• 405058-54-0 3-(hydroxymethyl)-N-phenylbenzenesulfonamide 
• 405058-55-1 3-formyl-N-phenylbenzene-1-sulfonamide 
• 412269-00-2 C₁₅H₁₃NO₄S 
• 414864-00-9 N-hydroxy-3-(3-phenylaminosulfonylphenyl)acrylamide 
• 866324-02-9 methyl 3-[(phenylamino)sulfonyl]benzenecarboxylate 
• 63555-50-0 methyl 3-chlorosulfonylbenzoate 

Relevant academic research and scientific papers

Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer

Nicotinamide phosphoribosyltransferase (NAMPT) has emerged as a promising target for the discovery of anticancer drugs. Based on NAMPT inhibitor FK866 that has been advanced into phase II trial, we identified a trans-3-(pyridin-3-yl)acrylamide compound 13 incorporating with a biarylsulfanilamide moiety as a new NAMPT inhibitor. Further structure-activity relationship (SAR) exploration led to additional biarylsulfanilamide-derived compounds with high in vitro NAMPT inhibitory potency and antiproliferative activity. In particular, compound 23, the most potent NAMPT inhibitor (IC50 = 5.08 nM), showed single-digit nanomolar antiproliferative activity against DU145, Hela, and H1975 cells with IC50 values of 2.90 nM, 2.34 nM, and 2.24 nM, respectively, and even subnanomolar level against K562, MCF-7, and HUH7 cells with IC50 values of 0.46 nM, 0.23 nM and 0.53 nM, respectively. Our findings provided promising lead compounds for the discovery of more potent NAMPT inhibitors as anticancer drugs.

Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors

In the past decade, although research and development of histone deacetylase (HDAC) inhibitors as therapeutic agents have achieved great accomplishments, especially in oncology field, there is still an urgent need for the discovery of isoform-selective HDAC inhibitors considering the side effects caused by nonselective HDAC inhibitors. HDAC8, a unique class I zinc-dependent HDAC, is becoming a potential target in cancer and other diseases. In the current study, a novel series of N-hydroxy-3-sulfamoylbenzamide-based HDAC8 selective inhibitors (12a-12p) were designed and synthesized, among which compounds 12a, 12b and 12c exhibited potent HDAC8 inhibition with two-digit nanomolar IC50 values, and considerable selectivity over HDAC2 (>180-fold) and HDAC6 (～30-fold) which was confirmed by western blot analysis. It is worth noting that 12a, 12b and 12c displayed highly selective anti-proliferative activity to T-cell leukemia cell lines Jurkat, Molt-4 and neuroblastoma cell line SK-N-BE-(2). Such selective cytotoxicity was also observed in the well-known HDAC8 selective inhibitor PCI-34051 but not in the pan-HDAC inhibitors SAHA and PXD101, indicating that HDAC8 selective inhibitor should have preferable benefit-risk profile in comparison with pan-HDAC inhibitor. Finally, the HDAC8 selectivity of 12a, 12b and 12c was rationalized by molecular docking study.

Histone deacetylase 8 selective inhibitor, as well as preparation method and application thereof

The invention discloses a histone deacetylase 8 selective inhibitor, as well as a preparation method and application thereof. The histone deacetylase 8 selective inhibitor has a structure as shown ina general formula (I) or (II) below. The invention further provides a preparation method of the compound and application in preparing medicines for preventing or treating diseases relevant to histonedeacetylase 8 (HDAC8) activity abnormality.

A he belli department is suitable for industrial production of synthetic method

The invention provides an improved belinostatsynthesis method. According to the method, sodium m-carboxyl benzenesulfonate is taken as a starting material, and belinostat is prepared through six steps of esterification, acylation and aniline condensation, reduction, oxidation, Wittig-Horner condensation and hydrolysis as well as acylation and hydroxylamine condensation. With the adoption of the method, the production time is shortened, the reaction yield is increased, the production safety is enhanced, the environmental pollution is reduced, and the method is more suitable for industrial production.