title: Combinatorial synthesis and screening of a chemical library of 1,4-dihydropyridine calcium channel blockers.
abstract: Solid-phase synthesis of a 300-member pharmacophore library of 1,4-dihydropyridines from keto ester, diketone and aldehyde building blocks on a cleavable amine polymeric support is described. Screening and serial deconvolution of the combinatorial library has resulted in identification of known and new potent calcium channel blockers.
authors.affiliation: Affymix Research Institute, Santa Clara, CA 95051, USA.
authors.forename: M F
authors.initials: MF
authors.lastname: Gordeev
authors.forename: D V
authors.initials: DV
authors.lastname: Patel
authors.forename: B P
authors.initials: BP
authors.lastname: England
authors.forename: S
authors.initials: S
authors.lastname: Jonnalagadda
authors.forename: J D
authors.initials: JD
authors.lastname: Combs
authors.forename: E M
authors.initials: EM
authors.lastname: Gordon
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D002121:Calcium Channel Blockers / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D015220:Calcium Channels / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D004095:Dihydropyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D066298:In Vitro Techniques; D009568:Nitrendipine / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats
chemical_list: D002121:Calcium Channel Blockers; D015220:Calcium Channels; D004095:Dihydropyridines; C038806:1,4-dihydropyridine; D009568:Nitrendipine