Syntheses and biological activity of bisdaunorubicins.
To study the length and flexibility of the linkers between two monomers of bisdaunorubicins for their activity against cancer cells, seven bisdaunorubicins were rationally designed and synthesized through click chemistry. Their cytotoxicity was tested in leukemia cells with MTS assay. The results showed that the compounds with short linkers exhibited higher activity than the compounds with long linkers, while the flexibility of the linker also contributed to their activity. These results indicated that the length and flexibility of the linkers between two monomers in bisdaunorubicins are very critical to maintain their activity against cancer cells.
Zhang
Guisheng
G
Department of Chemistry and Biochemistry, The Ohio State University, Columbus, OH 43210, USA.
Fang
Lanyan
L
Zhu
Lizhi
L
Sun
Duxin
D
Wang
Peng George
PG
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003630:Daunorubicin / Q000138:chemical synthesis* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020014:K562 Cells; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
D000970:Antineoplastic Agents; D003630:Daunorubicin