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Bioorg Med Chem Lett ; 14(11): 2829-33, 2004 Jun 07.
Article in English | MEDLINE | ID: mdl-15125941

ABSTRACT

In our investigations to synthesize inhibitors of smooth muscle cell (SMC) proliferation, compound 6a displayed submicromolar activity in in vitro antiproliferative assays and reduced intimal thickening using a rat balloon angioplasty model via i.v. administration. In order to identify analogs that could be administered orally, the chemical instability of the C-4',6' acetal of compound 6a was addressed. Several novel variants with increased acid stability and comparable in vitro activity were prepared.


Subject(s)
Maltose/pharmacology , Muscle, Smooth, Vascular/drug effects , Angioplasty, Balloon/adverse effects , Animals , Benzyl Compounds/chemical synthesis , Benzyl Compounds/pharmacology , Cell Proliferation/drug effects , Drug Stability , Hydrogen-Ion Concentration , Male , Maltose/chemical synthesis , Models, Animal , Muscle, Smooth, Vascular/injuries , Muscle, Smooth, Vascular/pathology , Rats , Rats, Sprague-Dawley , Structure-Activity Relationship
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