51-08-1Relevant articles and documents
Comparative study of dG affinity vs. DNA methylation modulating properties of side chain derivatives of procainamide: Insight into its DNA hypomethylating effect
Gawade,Chakravarty,Debgupta,Sangtani,Narwade,Gonnade,Puranik,Deobagkar
, p. 5350 - 5358 (2016/02/05)
Procainamide derivatives have been synthesized to investigate the role of side chains in modulating the DNA methylation level in cancer cells and gain insight into its mechanism of action. The synthesized derivatives comprised of flexible (dimethyl), cons
Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors
Lawrence, Harshani R.,Martin, Mathew P.,Luo, Yunting,Pireddu, Roberta,Yang, Hua,Gevariya, Harsukh,Ozcan, Sevil,Zhu, Jin-Yi,Kendig, Robert,Rodriguez, Mercedes,Elias, Roy,Cheng, Jin Q.,Sebti, Sa?d M.,Schonbrunn, Ernst,Lawrence, Nicholas J.
, p. 7392 - 7416 (2012/11/07)
The o-carboxylic acid substituted bisanilinopyrimidine 1 was identified as a potent hit (Aurora A IC50 = 6.1 ± 1.0 nM) from in-house screening. Detailed structure-activity relationship (SAR) studies indicated that polar substituents at the para position of the B-ring are critical for potent activity. X-ray crystallography studies revealed that compound 1 is a type I inhibitor that binds the Aurora kinase active site in a DFG-in conformation. Structure-activity guided replacement of the A-ring carboxylic acid with halogens and incorporation of fluorine at the pyrimidine 5-position led to highly potent inhibitors of Aurora A that bind in a DFG-out conformation. B-Ring modifications were undertaken to improve the solubility and cell permeability. Compounds such as 9m with water-solubilizing moieties at the para position of the B-ring inhibited the autophosphorylation of Aurora A in MDA-MB-468 breast cancer cells.
NOVEL CARBOXAMIDE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS
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Page/Page column 43, (2008/06/13)
Novel compounds of formula (I) which modulate MCH activity are disclosed, in which A is a linker; B is a connecting moiety; Ar1 and Ar2 are aryl or heteroaryl groups; R1 and R2 are hydrogen, halogen atoms, CF3, OCF3/