A non-crosslinking platinum-acridine hybrid agent shows enhanced cytotoxicity compared to clinical BCNU and cisplatin in glioblastoma cells.
Using clonogenic survival assays, we demonstrated that a new platinum-acridine hybrid agent, PT-ACRAMTU, is cytotoxic in SNB19 and U87MG glioblastoma cells at low-micromolar concentrations. PT-ACRAMTU is more cytotoxic than ACRAMTU (the platinum-free acridine), acts in a time and dose dependent manner, and appears to generate an apoptotic response in both cell lines on the basis of increased caspase-3 activity.
Hess
Suzanne M
SM
Department of Radiation Oncology, Wake Forest University School of Medicine, Winston-Salem, NC 27157, USA.
Anderson
Joel G
JG
Bierbach
Ulrich
U
D000166:Acridines / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D002330:Carmustine / Q000494:pharmacology* / Q000633:toxicity; D053148:Caspase 3; D020169:Caspases / Q000378:metabolism; D002460:Cell Line; D002945:Cisplatin / Q000494:pharmacology* / Q000633:toxicity; D003432:Cross-Linking Reagents / Q000494:pharmacology / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005909:Glioblastoma / Q000473:pathology; D020128:Inhibitory Concentration 50; D009944:Organoplatinum Compounds / Q000494:pharmacology / Q000633:toxicity; D010984:Platinum / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity
D000166:Acridines; D003432:Cross-Linking Reagents; D009944:Organoplatinum Compounds; D010984:Platinum; D053148:Caspase 3; D020169:Caspases; D002945:Cisplatin; D002330:Carmustine