title: Stability studies of C-4',6' acetal benzylmaltosides synthesized as inhibitors of smooth muscle cell proliferation.
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.
authors.affiliation: Chemical and Screening Sciences Department, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. mayers@wyeth.com
authors.forename: Scott C
authors.initials: SC
authors.lastname: Mayer
authors.forename: William
authors.initials: W
authors.lastname: Gallaway
authors.forename: John
authors.initials: J
authors.lastname: Kulishoff
authors.forename: Maisheng
authors.initials: M
authors.lastname: Yin
authors.forename: Vidya
authors.initials: V
authors.lastname: Gadamasetti
authors.forename: Robert
authors.initials: R
authors.lastname: Mitchell
mesh_terms: D000800:Angioplasty, Balloon / Q000009:adverse effects; D000818:Animals; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D008297:Male; D008320:Maltose / Q000138:chemical synthesis / Q000494:pharmacology*; D023421:Models, Animal; D009131:Muscle, Smooth, Vascular / Q000187:drug effects* / Q000293:injuries / Q000473:pathology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D001593:Benzyl Compounds; D008320:Maltose