PEG conjugates of potent I-4 integrin inhibitors, maintaining sustained levels and bioactivity in vivo, following subcutaneous administration

Mitsunobu reactions were employed to link t-butyl esters of I-4 integrin inhibitors at each of the termini of a three-arm, 40 kDa, branched PEG. Cleavage of the t-butyl esters using HCO2H provided easily isolated PEG derivatives, which are potent I-4 integrin inhibitors, and which achieve sustained...

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Published inBioorganic & medicinal chemistry letters Vol. 23; no. 14; pp. 4117 - 4119
Main Authors Smith, Jenifer, Rossiter, Kassandra, Semko, Christopher, Xu, Ying-Zi, Quincy, David, Jagodzinski, Jacek, Dappen, Michael, Konradi, Andrei, Vandevert, Christopher, Garrido, Caroline, Mao, Wenxian, Pablo, F, Wipke, Brian, Dofiles, Lilibeth, Wadsworth, Angie, Peterson, Eric, Lorenzana, Carlos, Simmonds, Stellanie, Messersmith, Elizabeth, Bard, Frederique, Pleiss, Michael, Yednock, Ted
Format Journal Article
LanguageEnglish
Published 01.07.2013
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Esters
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Summary:Mitsunobu reactions were employed to link t-butyl esters of I-4 integrin inhibitors at each of the termini of a three-arm, 40 kDa, branched PEG. Cleavage of the t-butyl esters using HCO2H provided easily isolated PEG derivatives, which are potent I-4 integrin inhibitors, and which achieve sustained levels and bioactivity in vivo, following subcutaneous administration to rats.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-1
ISSN:0960-894X
DOI:10.1016/j.bmcl.2013.05.048