title: Selective apoptosis-inducing activity of crinum-type Amaryllidaceae alkaloids.
abstract: The selective apoptosis-inducing activity of Amaryllidaceae alkaloids belonging to the crinane-type is reported. A mini-library of natural and synthetic crinane alkaloids was assembled. Biological screening indicated crinamine 4 and haemanthamine 9 to be potent inducers of apoptosis in tumour cells at micromolar concentrations. Structure-activity relationships demonstrated the requirement for both an alpha-C2 bridge and a free hydroxyl at the C-11 position as pharmacophoric requirements for this activity.
authors.affiliation: Department of Chemistry, McMaster University, 1280 Main Street West, Hamilton, Ont., Canada L8S 4M1.
authors.forename: James
authors.initials: J
authors.lastname: McNulty
authors.forename: Jerald J
authors.initials: JJ
authors.lastname: Nair
authors.forename: Carles
authors.initials: C
authors.lastname: Codina
authors.forename: Jaume
authors.initials: J
authors.lastname: Bastida
authors.forename: Siyaram
authors.initials: S
authors.lastname: Pandey
authors.forename: Jenny
authors.initials: J
authors.lastname: Gerasimoff
authors.forename: Carly
authors.initials: C
authors.lastname: Griffin
mesh_terms: D047151:Amaryllidaceae Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D002460:Cell Line; D045744:Cell Line, Tumor; D031407:Crinum; D004305:Dose-Response Relationship, Drug; D006801:Humans; D019668:Liliaceae / Q000737:chemistry*; D015394:Molecular Structure
chemical_list: D047151:Amaryllidaceae Alkaloids; D000972:Antineoplastic Agents, Phytogenic; C411129:crinamine