Synthesis and characterization of BODIPY-labeled colchicine.
Two BODIPY-labeled colchicine derivatives were synthesized and shown to bind to tubulin but only partially inhibit tubulin polymerization in the presence of GTP. Cytotoxicity studies were carried out in HeLa, HepG2, Raji and Vero cells. Apoptosis-inducing properties were determined by caspase 3/7 activity and flow cytometry and interactions between the derivatives and tubulin were verified by fluorescence microscopy of living cells.
Arnold
Leggy A
LA
St. Jude Children's Research Hospital, Department of Chemical Biology and Therapeutics, 332 N. Lauderdale St., Mail Stop 1000, Memphis, TN 38105-2794, USA.
Ranaivo
Patricia
P
Guy
R Kiplin
RK
D000818:Animals; D001896:Boron Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D003078:Colchicine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008856:Microscopy, Fluorescence; D008870:Microtubules / Q000187:drug effects; D015394:Molecular Structure; D050257:Tubulin Modulators / Q000737:chemistry* / Q000494:pharmacology; D014709:Vero Cells
C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D050257:Tubulin Modulators; D003078:Colchicine