title: New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.
abstract: The 70% aqueous methanolic extract of the Chinese plant Aristolochia manshuriensis was found to contain two novel substituted phenanthrene compounds, SCH 546909 (1), and another phenanthrene glycoside (2). The structures of 1 and 2 were established based on NMR studies. They were identified as inhibitors of the CDK2 enzyme. Compound 1 was found to be a potent inhibitor of the CDK2 enzyme with an IC50 of 140 nM, whereas compound 2 was found to be less active with an IC50 of >10 microM.
authors.affiliation: Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. vinod.hegde@spcorp.com
authors.forename: Vinod R
authors.initials: VR
authors.lastname: Hegde
authors.forename: Scott
authors.initials: S
authors.lastname: Borges
authors.forename: Mahesh
authors.initials: M
authors.lastname: Patel
authors.forename: Pradip R
authors.initials: PR
authors.lastname: Das
authors.forename: Bonnie
authors.initials: B
authors.lastname: Wu
authors.forename: Vincent P
authors.initials: VP
authors.lastname: Gullo
authors.forename: Tze-Ming
authors.initials: TM
authors.lastname: Chan
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D030022:Aristolochia / Q000737:chemistry*; D051357:Cyclin-Dependent Kinase 2 / Q000037:antagonists & inhibitors*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D006027:Glycosides / Q000737:chemistry* / Q000494:pharmacology; D006576:Heterocyclic Compounds, 4 or More Rings / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D000432:Methanol / Q000737:chemistry; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry*; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004365:Drugs, Chinese Herbal; D006027:Glycosides; D006576:Heterocyclic Compounds, 4 or More Rings; D010936:Plant Extracts; C549644:SCH 546909; D014867:Water; C495894:CDK2 protein, human; D051357:Cyclin-Dependent Kinase 2; D000432:Methanol