5101-00-8Relevant academic research and scientific papers
Synthesis and biological evaluations of 1,2-diaryl pyrroles as analogues of combretastatin A-4
Sun, Jun,Chen, Lei,Liu, Chunjiang,Wang, Zhan,Zuo, Daiying,Pan, Jiatong,Qi, Huan,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 1541 - 1547 (2016/02/05)
A series of novel 1,2-diaryl pyrroles as analogues of combretastatin A-4 (CA-4, 1a) were synthesized and evaluated for their antitumour potential against three cancer cell lines. Most compounds exhibited growth inhibition against all of the cancer cell lines. Compound 7q not only exhibited prominent antitumour efficacy with IC50 values of 0.390 μm in SGC-7901, 0.070 μm in HT-1080 and 0.045 μm in KB cell lines but also showed low activity with IC50 values of 30.08 μm in normal L929 cell line. Moreover, compound 7q inhibited tubulin polymerization into microtubules and caused microtubule destabilization. A molecular docking study of 7q was performed to determine its binding mode at the colchicine site in the tubulin dimer. 1,2-Diaryl pyrroles as combretastatin A-4 analogues were synthesized and evaluated for anti-proliferative activities. Compound 7q exhibited antitubulin activity.
Method for preparing chiral diphosphines
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, (2008/06/13)
The invention concerns a method for preparing a compound of formula (1) wherein: A represents naphthyl or phenyl optionally substituted; and Ar1, Ar2independently represent a saturated or aromatic carbocyclic group, optionally substituted.
Asymmetric hydrogenation method of a ketonic compound and derivative
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, (2008/06/13)
The present invention relates to a process for the asymmetric hydrogenation of a ketonic compound and derivative. The invention relates to the use of optically active metal complexes as catalysts for the asymmetric hydrogenation of a ketonic compound and derivative. The process for the asymmetric hydrogenation of a ketonic compound and derivative is characterized in that the asymmetric hydrogenation of said compound is carried out in the presence of an effective amount of a metal complex comprising as ligand an optically active diphosphine corresponding to one of the following formulae: STR1
Synthesis and PAF antagonist activity of some 2,5-diaryltetrahydrofurans incorporating PAF-like functional groups
Smith,Blackwell,Demaine,Garland,Hodson,Hyde,Parke,Rose,Sawyer,Tilling
, p. 347 - 358 (2007/10/03)
This paper describes the synthesis and structure-activity relationships of a series of 2,5-diaryltetrahydrofurans, as specific and potent antagonists at the rabbit washed platelet activating factor (PAF) receptor. The methoxyl groups in the known PAF antagonist L-652,731 were replaced with functional groups present in PAF and in the 'PAF-like' antagonists. Activity was generally retained or enhanced when one aryl ring in L-652,731 was elaborated; however incorporation of these functional groups into both of the aryl rings greatly reduced or abolished activity. These results are discussed in relation to a putative model for the PAF receptor.
