Bioorganic and Medicinal Chemistry Letters p. 2855 - 2858 (1998)
Update date:2022-08-02
Topics:
Poncet, Joel
Hortala, Laurent
Busquet, Magali
Gueritte-Voegelein, Francoise
Thoret, Sylvie
Pierre, Alain
Atassi, Ghanem
Jouin, Patrick
A cyclic analog of the natural antiproliferative compound dolastatin 10 was synthesized by introducing an ester link between the N- and C-terminal residues which were modified accordingly. The final macrolactonization was performed by using isopropenyl chloroformate and DMAP as reagents. This analog exhibits submicromolar antiproliferative activity against the L1210 and HT29 cell lines and inhibits in vitro tubulin polymerization (IC50, 39 μM).
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