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Stability studies of C-4',6' acetal benzylmaltosides synthesized as inhibitors of smooth muscle cell proliferation
Authors:Mayer Scott C  Gallaway William  Kulishoff John  Yin Maisheng  Gadamasetti Vidya  Mitchell Robert
Affiliation:Chemical and Screening Sciences Department, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. mayers@wyeth.com
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.
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