- Syntheses of a radiolabelled CXCR2 antagonist AZD5069 and its major human metabolite
-
The CXCR2 antagonist AZD5069 has been synthesized in tritium and carbon-14-labelled forms. [3H]AZD5069 was prepared via reductive dehalogenation of an iodinated precursor with tritium gas to provide material with a specific activity of 25.1 Ci/
- Hickey, Michael J.,Allen, Paul H.,Caffrey, Moya,Hansen, Peter,Kingston, Lee P.,Wilkinson, David J.
-
-
Read Online
- Measurements of weak halogen bond donor abilities with tridentate anion receptors
-
The chelate effect of a tridentate receptor is exploited to determine halogen bonding association constants that vary by several orders of magnitude, including interactions of weak donors for which thermodynamic data were not previously available. Free en
- Dimitrijevic, Elena,Kvak, Olga,Taylor, Mark S.
-
supporting information; experimental part
p. 9025 - 9027
(2011/02/16)
-
- Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N′-(2-fluoro-5- methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor
-
In our continued efforts to search for potent and novel receptor tyrosine kinase (RTK) inhibitors as potential anticancer agents, we discovered, through a structure-based design, that 3-aminoindazole could serve as an efficient hinge-binding template for kinase inhibitors. By incorporating an N,N′-diaryl urea moiety at the C4-position of 3-aminodazole, a series of RTK inhibitors were generated, which potently inhibited the tyrosine kinase activity of the vascular endothelial growth factor receptor and the platelet-derived growth factor receptor families. A number of compounds with potent oral activity were identified by utilizing an estradiol-induced mouse uterine edema model and an HT1080 human fibrosarcoma xenograft tumor model. In particular, compound 17p (ABT-869) was found to possess favorable pharmacokinetic profiles across different species and display significant tumor growth inhibition in multiple preclinical animal models.
- Dai, Yujia,Hartandi, Kresna,Ji, Zhiqin,Ahmed, Asma A.,Albert, Daniel H.,Bauch, Joy L.,Bouska, Jennifer J.,Bousquet, Peter F.,Cunha, George A.,Glaser, Keith B.,Harris, Christopher M.,Hickman, Dean,Guo, Jun,Li, Junling,Marcotte, Patrick A.,Marsh, Kennan C.,Moskey, Maria D.,Martin, Ruth L.,Olson, Amanda M.,Osterling, Donald J.,Pease, Lori J.,Soni, Niru B.,Stewart, Kent D.,Stoll, Vincent S.,Tapang, Paul,Reuter, David R.,Davidsen, Steven K.,Michaelides, Michael R.
-
p. 1584 - 1597
(2008/02/01)
-