Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
18
pubmed:dateCreated
2010-9-16
pubmed:abstractText
?-Sulfone-?-piperidine and ?-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP's-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. ?-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while ?-piperidine and ?-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
1520-4804
pubmed:author
pubmed-author:BartaThomas ETE, pubmed-author:BeckerDaniel PDP, pubmed-author:BedellLouis JLJ, pubmed-author:BoehmTerri LTL, pubmed-author:BondBrian RBR, pubmed-author:CarrollJefferyJ, pubmed-author:CarronChris PCP, pubmed-author:DecrescenzoGary AGA, pubmed-author:EastonAlan MAM, pubmed-author:FreskosJohn NJN, pubmed-author:Funckes-ShippyChris LCL, pubmed-author:HeronMarciaM, pubmed-author:HockermanSusanS, pubmed-author:HowardCarol PearcyCP, pubmed-author:KieferJames RJR, pubmed-author:LiMadeleine HMH, pubmed-author:MathisKarl JKJ, pubmed-author:McDonaldJoseph JJJ, pubmed-author:MehtaPramod PPP, pubmed-author:MunieGrace EGE, pubmed-author:RodT OTO, pubmed-author:SunyerTeresaT, pubmed-author:SwearingenCraig ACA, pubmed-author:VillamilClara ICI, pubmed-author:WelschDeanD, pubmed-author:WilliamsJennifer MJM, pubmed-author:YuYingY
pubmed:issnType
Electronic
pubmed:day
23
pubmed:volume
53
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6653-80
pubmed:meshHeading
pubmed-meshheading:20726512-Animals, pubmed-meshheading:20726512-Anti-Inflammatory Agents, pubmed-meshheading:20726512-Antineoplastic Agents, pubmed-meshheading:20726512-Biological Availability, pubmed-meshheading:20726512-Cardiovascular Agents, pubmed-meshheading:20726512-Cartilage, Articular, pubmed-meshheading:20726512-Cattle, pubmed-meshheading:20726512-Crystallography, X-Ray, pubmed-meshheading:20726512-Humans, pubmed-meshheading:20726512-Hydroxamic Acids, pubmed-meshheading:20726512-Hypertrophy, Left Ventricular, pubmed-meshheading:20726512-Macaca fascicularis, pubmed-meshheading:20726512-Matrix Metalloproteinase 1, pubmed-meshheading:20726512-Matrix Metalloproteinases, pubmed-meshheading:20726512-Mice, pubmed-meshheading:20726512-Mice, Nude, pubmed-meshheading:20726512-Models, Molecular, pubmed-meshheading:20726512-Molecular Structure, pubmed-meshheading:20726512-Piperidines, pubmed-meshheading:20726512-Pyrans, pubmed-meshheading:20726512-Rats, pubmed-meshheading:20726512-Structure-Activity Relationship, pubmed-meshheading:20726512-Sulfones, pubmed-meshheading:20726512-Xenograft Model Antitumor Assays
pubmed:year
2010
pubmed:articleTitle
Orally active MMP-1 sparing ?-tetrahydropyranyl and ?-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
pubmed:affiliation
Pfizer Research, 700 Chesterfield Village Parkway, St. Louis, Missouri 63198, USA. dbecke3@luc.edu
pubmed:publicationType
Journal Article