209784-84-9

Upstream product

• 150-13-0 4-amino-benzoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 56-91-7 p-aminomethylbenzoic acid 
• 130029-61-7 4-[[(2,2,2-trifluoroacetyl)amino]methyl]benzoic acid 
• 146651-75-4 tert–butyl (2–aminophenyl)carbamate 

Downstream Products

• 209784-85-0 [2-(4-aminomethylbenzoylamino)phenyl]carbamic acid tert-butyl ester 
• 1448350-40-0 tert-butyl N-{2-[4-(isothiocyanatomethyl)benzamido]phenyl}carbamate 
• 1448350-41-1 tert-butyl N-(2-{4-[({[(1S)-2-hydroxy-1-phenylethyl]carbamothioyl}amino)methyl]benzamido}phenyl)carbamate 
• 1448350-42-2 tert-butyl N-(2-{4-[({[(1R)-2-hydroxy-1-phenylethyl]carbamothioyl}amino)methyl]benzamido}phenyl)carbamate 
• 1448350-43-3 (S)-tert-butyl N-(2-(4-((3-(2-hydroxy-1-(4-hydroxyphenyl)ethyl)thioureido)methyl)benzamido)phenyl)carbamate 
• 1448350-44-4 tert-butyl N-(2-{4-[({[(2S)-1-hydroxy-3-phenylpropan-2-yl]carbamothioyl}amino)methyl]benzamido}phenyl)carbamate 
• 1448350-45-5 tert-butyl N-(2-{4-[({[(2R)-1-hydroxy-3-phenylpropan-2-yl]carbamothioyl}amino)methyl]benzamido}phenyl)carbamate 
• 1448350-46-6 (S)-tert-butyl N-(2-(4-((3-(2-hydroxy-2-phenylethyl)thioureido)methyl)benzamido)phenyl)carbamate 
• 1448350-47-7 (R)-tert-butyl N-(2-(4-((3-(2-hydroxy-2-phenylethyl)thioureido)methyl)benzamido)phenyl)carbamate 
• 1448350-48-8 tert-butyl N-(2-(4-((3-((1R,2S)-2-hydroxy-1,2-diphenylethyl)thioureido)methyl)benzamido)phenyl)carbamate 
• 1448350-49-9 tert-butyl N-(2-(4-((3-((1S,2R)-2-hydroxy-1,2-diphenylethyl)thioureido)methyl)benzamido)phenyl)carbamate 
• 1448350-50-2 N-(2-aminophenyl)-4-({[(4S)-4-phenyl-4,5-dihydro-1,3-thiazol-2-yl]amino}methyl)benzamide 
• 1448350-51-3 N-(2-aminophenyl)-4-({[(4R)-4-phenyl-4,5-dihydro-1,3-thiazol-2-yl]amino}methyl)benzamide 
• 1448350-52-4 (S)-N-(2-aminophenyl)-4-(((4-(4-hydroxyphenyl)-4,5-dihydrothiazol-2-yl)amino)methyl)benzamide 

Relevant academic research and scientific papers

Discovery of multi-target anticancer agents based on HDAC inhibitor MS-275 and 5-FU

Histone deacetylases (HDACs) inhibitors have multiple effects targeting the cancer cells and have become one of the promising cancer therapeutics with possibly broad applicability. Combination of HDAC inhibitors with the cytotoxic fluorouracil (5-FU) show

CRYSTALLINE FORMS OF ENTINOSTAT

Entinostat is a histone deacetylase inhibitor undergoing clinical investigation in multiple types of solid tumors, such as breast cancer, and hematologic cancers. Crystalline form D and E of Entinostat and crystal form A in high crystal purity are provided. Crystalline form D can be obtained in high chemical purity, exhibits improved water solubility and allows efficient purification of Entinostat with removal of coloured impurities. Processes for the preparation of such crystalline forms and of form A with improved chemical and crystal purity are also provided.

Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit

The synthesis of a novel series of potent chiral inhibitors of histone deacetylase (HDAC) is described that contain a heterocyclic capping group and a N-(2-aminophenyl)benzamide unit that binds in the active site. In vitro assays for the inhibition of HDAC1, HDAC2, HDAC3-NCoR1, and HDAC8 by the N-(2-aminophenyl)benzamide 24a gave respective IC50 values of 930, 85, 12, and 4100 nM, exhibiting class I selectivity and potent inhibition of HDAC3-NCoR1. Both imidazolinone and thiazoline rings are shown to be effective replacements for the pyrimidine ring present in many other 2-(aminophenyl) benzamides previously reported, an example of each ring system at 1 μM causing an increase in histone H3K9 acetylation in the human cell lines Jurkat and HeLa and an increase in cell death consistent with induction of apoptosis. Inhibition of the growth of MCF-7, A549, DU145, and HCT116 cell lines by 24a was observed, with respective IC50 values of 5.4, 5.8, 6.4, and 2.2 mM.