title: Triaryl methane derivatives as antiproliferative agents.
abstract: Clotrimazole (CLT) 1, a synthetic anti-fungal imidazole derivative, inhibits tumor cell proliferation and angiogenesis. In the current study, flow cytometric analysis demonstrated that the decrease in tumor cell growth by CLT 1 was associated with inhibition of cell cycle progression at the G(1)-S phase transition, resulting in G(0)-G(1) arrest. A series of CLT 1 analogues has been generated in order to develop CLT 1 derivatives that are devoid of the imidazole moiety which is responsible for the hepatoxicity associated with CLT 1 while retaining CLT 1 efficacy. The majority of these analogues demonstrate in vitro antiproliferative activity ranging from submicromolar to micromolar concentrations.
authors.affiliation: Lorus Therapeutics Inc., 2Meridian Road, M9W 4Z7, Toronto, ON, Canada.
authors.forename: Raed A
authors.initials: RA
authors.lastname: Al-Qawasmeh
authors.forename: Yoon
authors.initials: Y
authors.lastname: Lee
authors.forename: Ming Yu
authors.initials: MY
authors.lastname: Cao
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Gu
authors.forename: Aikaterini
authors.initials: A
authors.lastname: Vassilakos
authors.forename: Jim A
authors.initials: JA
authors.lastname: Wright
authors.forename: Aiping
authors.initials: A
authors.lastname: Young
mesh_terms: D000818:Animals; D002455:Cell Division / Q000187:drug effects / Q000502:physiology; D045744:Cell Line, Tumor; D003022:Clotrimazole / Q000031:analogs & derivatives / Q000494:pharmacology; D006131:Growth Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008697:Methane / Q000031:analogs & derivatives* / Q000494:pharmacology*; D051379:Mice; D041681:NIH 3T3 Cells
chemical_list: D006131:Growth Inhibitors; D003022:Clotrimazole; D008697:Methane