Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents.

@article{Lisowski2004DesignSA,
  title={Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents.},
  author={Vincent Lisowski and St{\'e}phane L{\'e}once and Laurence Kraus-Berthier and Jana Sopkov{\'a}-de Oliveira Santos and Alain Pierre and Ghanem Atassi and D Caignard and Pierre Renard and Sylvain Rault},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 6},
  pages={1448-64}
}
Herein, we describe the structure-activity relationship study of a new 3-aryl-8H-thieno[2,3-b]pyrrolizin-8-one series of antitubulin agents. The pharmacological results from the National Cancer Institute in vitro human disease oriented tumor cell line screening allowed us to identify compound 1d (NSC 676693) as a very efficient antitumoral drug in all cancer cell lines tested. This prompted us to define the structural requirements essential for this antiproliferative activity. Among all… CONTINUE READING