- Identification of small molecule sulfonic acids as ecto-5'-nucleotidase inhibitors
-
Ecto-5'-Nucleotidase inhibitors have great potential as anti-tumor agents. We have investigated biochemical properties of human and rat ecto-5'-Nucleotidases and characterized 19 small molecule sulfonic acid derivatives as potential inhibitors of ecto-5'-Nucleotidases. We identified 11 potent inhibitors of human and rat ecto-5'-Nucleotidases and checked their selectivity. Compound 10 (Sodium 2,4-dinitrobenzenesulfonate) with Ki value of 0.66 μM and 19 (N-(4- sulfamoylphenylcarbamothioyl) pivalamide) with Ki value of 0.78 μM were identified as the most potent inhibitors for human and rat ecto-5'-Nucleotidase, respectively. The present compounds have low molecular weights, water solubility and equal potency as compared to the reported inhibitors.
- Raza, Rabia,Saeed, Aamer,Lecka, Joanna,Sévigny, Jean,Iqbal, Jamshed
-
p. 1133 - 1139
(2013/01/15)
-
- Polymorphic clopidogrel hydrogenesulphate form
-
Novel orthorombic polymorph of clopidogrel hydrogen sulfate or hydrogen sulfate of methyl (+)-(S)-α-(2-chlorophenyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-5-acetate and a process for its preparation.
- -
-
-
- Dibenzonaphthyrones
-
Dibenzonaphthyrone of formula (I) wherein A1and A2independently of each other are unsubstituted or mono- to tetra-substituted o-C6-C18arylene, with the proviso that formula (I) does not represent a dibenzonaphthyrone of the formula The invention further relates to processes for the preparation thereof, to the use thereof for colouring/pigmenting high-molecular-weight organic material and to substance compositions comprising dibenzonaphthyrones.
- -
-
-
- Action of Red Light on Solid (+)-10-Bromo-2-chloro-2-nitrosocamphane: (i) Nuclear and Electron Paramagnetic Resonance Studies; (ii) Reaction Products; (iii) Solid-state Photolysis Reaction Mechanisms
-
Photolysis of blue, solid (+)-10-bromo-2-chloro-2-nitrosocamphane (1) with red light produces two nitroxide radicals (2) and (3), 10-bromocamphor (4), a 10-bromo-2-chloro-2-nitrocamphane (5), a 2-chloro-5,5-dimethyl-1,2-dinitrobicyclooctane (6a), and a corresponding 1-nitrato-analogue (6b).E.p.r. spectra of (2) and (3) are described and interpreted.Analyses of the 1H n.m.r. spectra of compounds (1) and (5) show that n.m.r. method can be used to determine configurations at active XCCl (X = NO or NO2) centres of gem-chloronitroso and gem-chloronitro derivatives of the terpenes.The combination of chemical and spectroscopic evidence enables some of the steps involved in the solid-state red photolysis reaction of (1) to be unravelled.
- Majeed, Nesreen N.,Porte, Andrew L.
-
p. 1139 - 1146
(2007/10/02)
-
- Process for the preparation of D(-)αphenylglycine
-
The invention provides a process for the preparation of D(-)αphenylglycine by resolution of DLαphenylglycine by means of D(+)camphorsulfonic acid. The present process enables the preparation of D(-)αphenylglycine at a minimum loss of the very expensive starting materials, such as DLαphenylglycine and D(+)camphorsulfonic acid. The salts produced in this process are precipitated from the resolution filtrate and the filtrate may be discarded as effluent water without any danger to the environment.
- -
-
-
