title: In vitro apoptotic activity of 2,2-diphenyl-1,3,2-oxazaborolidin-5-ones in L5178Y cells.
abstract: Compounds containing B-N bonds have shown interesting biological activity. One class of such molecules is the 2,2-diphenyl-1,3,2-oxazaborolidin-5-ones (3a-j), which contain a B-N bond, have an alpha-amino acid moiety in the heterocycle, and have an exocyclic moiety related to an amino acid. The purpose of this work was to determine the inhibitory effects of 3a-j on the proliferation of murine L5178Y lymphoma cells. A new five-membered heterocyclic nucleus with apoptotic activity was found. The target products showed potent cytotoxicity in the L5178Y cell line. Among them, 3a exhibited the highest antineoplastic activity in L5178Y cells with an IC(50) value of 22.5+/-0.2 microM.
authors.affiliation: Departamento de Bioquímica y Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina-IPN, México DF, México.
authors.forename: Benjamín
authors.initials: B
authors.lastname: Velasco
authors.forename: José G
authors.initials: JG
authors.lastname: Trujillo-Ferrara
authors.forename: Luis H Fabila
authors.initials: LH
authors.lastname: Castillo
authors.forename: René
authors.initials: R
authors.lastname: Miranda
authors.forename: Luvia E
authors.initials: LE
authors.lastname: Sánchez-Torres
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001896:Boron Compounds / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D053938:DNA Fragmentation; D004273:DNA, Neoplasm / Q000032:analysis; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005434:Flow Cytometry; D005562:Formazans / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007940:Leukemia L5178 / Q000378:metabolism / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D010718:Phosphatidylserines / Q000378:metabolism; D013778:Tetrazolium Salts / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D001896:Boron Compounds; D004273:DNA, Neoplasm; D005562:Formazans; D010718:Phosphatidylserines; D013778:Tetrazolium Salts; C079782:MTT formazan