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© Yang SI, Institut Pasteur
Publication : Bioconjugate chemistry

Optimized synthesis and enhanced efficacy of novel triplex-forming camptothecin derivatives based on gimatecan

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Bioconjugate chemistry - 01 Apr 2009

Vekhoff P, Halby L, Oussedik K, Dallavalle S, Merlini L, Mahieu C, Lansiaux A, Bailly C, Boutorine A, Pisano C, Giannini G, Alloatti D, Arimondo PB

Link to Pubmed [PMID] – 19309124

Bioconjug. Chem. 2009 Apr;20(4):666-72

Sequence-specific camptothecins are useful tools to inhibit specifically gene expression. The camptothecins are attached to the 3′ end of triplex-forming oligonucleotides (TFO), sequence-specific DNA ligands that position the camptothecin moiety exclusively in proximity to their binding site. We studied here different gimatecan derivatives or analogues, a potent lipophilic camptothecin compound in clinical trials. We optimized the synthesis procedure in order to increase the yields and the purity and obtain the conjugates on a large scale. The greatly improved synthesis is now based on the conjugation of a bromoalkyl analogue of gimatecan to the 3′ phosphorothioate of the TFO. We showed that the most efficient conjugate, both in vitro and in HeLa cells, bears the TFO on position 7 of the gimatecan analogue, and it is more efficient than the previous camptothecin conjugates. In addition, the gimatecan-like moiety at the 3′ end of the TFO protects from nuclease degradation.

https://www.ncbi.nlm.nih.gov/pubmed/19309124