title: Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis.
abstract: 4-Arylpyrano-[3,2-c]-pyridones have been prepared by a one-step cyclocondensation of 4-hydroxy-1,6-dimethylpyridin-2(1H)-one with various substituted benzaldehydes and malononitrile. These heterocycles exhibit micromolar and submicromolar antiproliferative activity in HeLa and induce apoptosis in Jurkat cell lines. Structure-activity studies performed on a small library of these compounds show a pronounced cytotoxicity enhancing effect of the bromo substituent at the meta position of the C4 aromatic moiety.
authors.affiliation: Department of Organic Chemistry, Timiryazev Agriculture Academy, Moscow 127550, Russia.
authors.forename: Igor V
authors.initials: IV
authors.lastname: Magedov
authors.forename: Madhuri
authors.initials: M
authors.lastname: Manpadi
authors.forename: Nikolai M
authors.initials: NM
authors.lastname: Evdokimov
authors.forename: Eerik M
authors.initials: EM
authors.lastname: Elias
authors.forename: Elena
authors.initials: E
authors.lastname: Rozhkova
authors.forename: Marcia A
authors.initials: MA
authors.lastname: Ogasawara
authors.forename: Jennifer D
authors.initials: JD
authors.lastname: Bettale
authors.forename: Nikolai M
authors.initials: NM
authors.lastname: Przheval'skii
authors.forename: Snezna
authors.initials: S
authors.lastname: Rogelj
authors.forename: Alexander
authors.initials: A
authors.lastname: Kornienko
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D019169:Jurkat Cells; D011728:Pyridones / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011728:Pyridones