618892-17-4Relevant academic research and scientific papers
Synthesis of MMP inhibitor radiotracer [11C]CGS 25966, a new potential PET tumor imaging agent
Fei, Xiangshu,Zheng, Qi-Huang,Liu, Xuan,Wang, Ji-Quan,Stone, K. Lee,Miller, Kathy D.,Sledge, George W.,Hutchins, Gary D.
, p. 343 - 351 (2007/10/03)
[11C]CGS 25966, a novel radiolabeled matrix metalloproteinase (MMP) inhibitor, has been synthesized for evaluation as new potential positron emission tomography (PET) tumor imaging agent. The precursor was labeled by [11C]methyl triflate through O-[11C]methylation method at the hydroxyl position of phenol under basic conditions and isolated by HPLC purification to produce pure target compound in 15-25% radiochemical yield, based on 11CO2, decay corrected to end of bombardment. Copyright
Discovery of CGS 27023A, a non, peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits
MacPherson, Lawrence J.,Bayburt, Erol K.,Capparelli, Michael P.,Carroll, Brian J.,Goldstein, Robert,Justice, Michael R.,Zhu, Lijuan,Hu, Shou-Ih,Melton, Richard A.,Fryer, Lynn,Goldberg, Ron L.,Doughty, John R.,Spirito, Salvatore,Blancuzzi, Vincent,Wilson, Doug,O'Byrne, Elizabeth M.,Ganu, Vishwas,Parker, David T.
, p. 2525 - 2532 (2007/10/03)
Structure-activity relationships of a lead hydroxamic acid inhibitor of recombinant human stromelysin were systematically defined by taking advantage of a concise synthesis that allowed diverse functionality to be explored at each position in a template. An ex vivo rat model and an in vivo rabbit model of stromelysin-induced cartilage degradation were used to further optimize these analogs for oral activity and duration of action. The culmination of these modifications resulted in CGS 27023A, a potent, orally active stromelysin inhibitor that blocks the erosion of cartilage matrix.
