In vitro apoptotic activity of 2,2-diphenyl-1,3,2-oxazaborolidin-5-ones in L5178Y cells.
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.
Velasco
Benjamín
B
Departamento de Bioquímica y Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina-IPN, México DF, México.
Trujillo-Ferrara
José G
JG
Castillo
Luis H Fabila
LH
Miranda
René
R
Sánchez-Torres
Luvia E
LE
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
D000970:Antineoplastic Agents; D001896:Boron Compounds; D004273:DNA, Neoplasm; D005562:Formazans; D010718:Phosphatidylserines; D013778:Tetrazolium Salts; C079782:MTT formazan