Borato-1,2-diaminocyclohexane platinum (II), a novel anti-tumor drug.
Borato-1,2-diaminocyclohexane platinum (II) (BDP) was synthesized and compared to cisplatin (cisPt) as a potential anti-tumor drug. BDP and cisPt (0.2-20 microM) dose-dependently inhibited DNA synthesis in L1210 murine leukemia cells, DU-145 prostate cancer cells, A549 lung carcinoma cells, and MCF-7 breast cancer cells, as judged by measuring [(3)H]-thymidine incorporation. BDP and cisPt induced killing of L1210 murine cells by 97 and 78%, respectively. The LD(50) was 35 and 14 mg/kg for BDP and cisPt, respectively. Interestingly, while cisPt (at optimal dose) induced a 100% increase in life span (ILS) of BDF1 mice bearing L1210 tumor cells, BDP (at optimal dose) induced a 200% increase in ILS in the same tumor model. In conclusion, BDP is a novel platinum derivative compound that appears more effective in increasing the ILS than cisplatin against the leukemia tumor mouse model.
Dibas
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A
Mary Kay Ash Institute for Cancer Research, St. Paul Medical Center, Dallas, Texas 75235, USA.
Howard
J
J
Anwar
S
S
Stewart
D
D
Khan
A
A
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001896:Boron Compounds / Q000494:pharmacology*; D004261:DNA Replication / Q000187:drug effects; D006801:Humans; D007928:Lethal Dose 50; D051379:Mice; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001896:Boron Compounds; D009944:Organoplatinum Compounds; C407358:borato-1,2-diaminocyclohexane platinum(II)