Bioorganic & Medicinal Chemistry Letters 2004-06-07

Stability studies of C-4',6' acetal benzylmaltosides synthesized as inhibitors of smooth muscle cell proliferation.

Scott C Mayer, William Gallaway, John Kulishoff, Maisheng Yin, Vidya Gadamasetti, Robert Mitchell

Index: Bioorg. Med. Chem. Lett. 14(11) , 2829-33, (2004)

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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.