title: 3,5-Bis-arylidene-1-methyl-4-piperidone methohalides and related compounds with activity against L 1210 cells and DNA binding properties.
abstract: A series of 3,5-bis-arylidene-1-methyl-4-piperidone methohalides 2 and two related analogues in general demonstrated activity against L 1210 leukemia cells in vitro and bound to a synthetic DNA, poly[d(AT)]. Plots of various physicochemical constants of the aromatic substituents in series 2 versus the IC50 figures revealed correlations between the aryl MR and pi values but not the sigma constants. The delta Tm values of six members of series 2 were correlated with the MR figures of the aryl substituents but not the sigma nor pi values of the aromatic atoms and groups. Some suggestions for future molecular modification with a view to increasing cytotoxicity are presented.
authors.affiliation: College of Pharmacy, University of Saskatchewan, Saskatoon, Canada.
authors.forename: J R
authors.initials: JR
authors.lastname: Dimmock
authors.forename: V K
authors.initials: VK
authors.lastname: Arora
authors.forename: H A
authors.initials: HA
authors.lastname: Semple
authors.forename: J S
authors.initials: JS
authors.lastname: Lee
authors.forename: T M
authors.initials: TM
authors.lastname: Allen
authors.forename: G Y
authors.initials: GY
authors.lastname: Kao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004273:DNA, Neoplasm / Q000187:drug effects / Q000378:metabolism*; D007939:Leukemia L1210 / Q000188:drug therapy*; D051379:Mice; D010881:Piperidones / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011728:Pyridones / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D001597:Benzylidene Compounds; D004273:DNA, Neoplasm; D010881:Piperidones; D011728:Pyridones