33681-23-1Relevant academic research and scientific papers
Synthesis and anticancer potential of novel xanthone derivatives with 3,6-substituted chains
Liu, Chaomei,Zhang, Mei,Zhang, Zhenhuan,Zhang, Steven B.,Yang, Shanmin,Zhang, Amy,Yin, Liangjie,Swarts, Steven,Vidyasagar, Sadasivan,Zhang, Lurong,Okunieff, Paul
, p. 4263 - 4271 (2016/08/23)
In an effort to develop new drug candidates with enhanced anticancer activity, our team synthesized and assessed the cytotoxicity of a series of novel xanthone derivatives with two longer 3,6-disubstituted amine carbonyl methoxy side chains on either benzene ring in selected human cancer cell lines. An MTT assay revealed that a set of compounds with lower IC50values than the positive control, 5-FU, exhibited greater anticancer effects. The most potent derivative (XD8) exhibited anticancer activity in MDA-MB-231, PC-3, A549, AsPC-1, and HCT116 cells lines with IC50values of 8.06, 6.18, 4.59, 4.76, and 6.09?μM, respectively. Cell cycle analysis and apoptosis activation suggested that the mechanism of action of these derivatives includes cell cycle regulation and apoptosis induction.
Synthesis, spectral studies and anti-inflammatory activity of glycolamide esters of niflumic acid as potential prodrugs
Gadad, Andanappa K.,Bhat, Shailija,Tegeli, Varsha S.,Redasani, Vivek V.
, p. 817 - 821 (2007/10/03)
In order to reduce the gastric irritation caused by direct contract mechanism of the carboxylic acid group, a series of glycolamide esters of niflumic (CAS 4394-00-7) (1) have been prepared as biolabile prodrugs by reacting appropriate 2-chloroacetamides with niflumic acid. The required 2-chloroacetamides were obtained by the condensation of chloroacetyl chloride and corresponding amine. Their structures were confirmed by UV, IR and 1H NMR spectra. Selected compounds were evaluated for anti-inflammatory activity in carrageenan induced paw oedema in rats at the doses of 45, 90 and 150 mg/kg b.w. Prodrugs showed comparable anti-inflammatory activity (67.1-79.4%) at 150 mg/kg b.w. with respect to niflumic acid (70.3%) at 45 mg/kg b.w., indicating moderate release of niflumic acid in vivo. The highest activity was observed with diethylamine (4) and pyrrolidine (9) derivatives.
LTA4 HYDROLASE INHIBITOR PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE
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, (2008/06/13)
The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an a
BENZOTHIAZEPINE AND BENZOXAZEPINE DERIVATIVES AS CHOLECYSTOKININ RECEPTOR ANTAGONISTS
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, (2008/06/13)
The present invention relates to novel substituted benzothiazepines and benzoxazepines of the formula STR1 wherein R 1, R 2, R. sup. 7, R 8, R 9 and X are as defined below, and to novel intermediates used in the synthesis of such compounds. Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.
LTA4 HYDROLASE INHIBITORS
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, (2008/06/13)
The present invention provides compounds of the formula Ar1?Q?Ar2?Y?R?Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an a
Amide phosphorothiolate herbicides
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, (2008/06/13)
The present invention relates to new herbicidal phosphorothioate (phosphorodithioate) derivatives and to preparation thereof.
