نتایج جستجو برای: phthalazine

تعداد نتایج: 192  

Journal: :Journal of medicinal chemistry 2010
Victor J Cee Laurie B Schenkel Brian L Hodous Holly L Deak Hanh N Nguyen Philip R Olivieri Karina Romero Annette Bak Xuhai Be Steve Bellon Tammy L Bush Alan C Cheng Grace Chung Steve Coats Patrick M Eden Kelly Hanestad Paul L Gallant Yan Gu Xin Huang Richard L Kendall Min-Hwa Jasmine Lin Michael J Morrison Vinod F Patel Robert Radinsky Paul E Rose Sandra Ross Ji-Rong Sun Jin Tang Huilin Zhao Marc Payton Stephanie D Geuns-Meyer

The discovery of aurora kinases as essential regulators of cell division has led to intense interest in identifying small molecule aurora kinase inhibitors for the potential treatment of cancer. A high-throughput screening effort identified pyridinyl-pyrimidine 6a as a moderately potent dual inhibitor of aurora kinases -A and -B. Optimization of this hit resulted in an anthranilamide lead (6j) ...

Journal: :Journal of analytical oncology 2012
Ingrid Cely Seang Yiv Qian Yin Anoush Shahidzadeh Li Tang Jianjun Cheng Fatih M Uckun

The pentapeptide mimic 1,4-bis(9-O-dihydroquinidinyl)phthalazine / hydroquinidine 1,4-phathalazinediyl diether ("compound 61") (C-61) is the first reported inhibitor targeting the P-site of SYK. Here we report a nanotechnology platform to target C-61 to mantle cell lymphoma (MCL) cells. Liposomal nanoparticles (NP) loaded with C-61 were prepared using the standard thin film evaporation method. ...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2004
R Scott Obach

The selective estrogen receptor modulator, raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with K(i) values of 0.87 to 1.4 nM. Inhibition was not time-dependent. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed ...

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