par Dasari, Ramesh;Banuls, Laetitia Moreno Y;Masi, Marco;Pelly, Stephen C;Mathieu, Véronique ;Green, Ivan R;van Otterlo, Willem A L;Evidente, Antonio;Kiss, Robert ;Kornienko, Alexander
Référence Bioorganic & medicinal chemistry letters, 24, 3, page (923-927)
Publication Publié, 2014-02
Référence Bioorganic & medicinal chemistry letters, 24, 3, page (923-927)
Publication Publié, 2014-02
Article révisé par les pairs
Résumé : | As a continuation of the studies aimed at the development of new anticancer agents derived from the Amaryllidaceae alkaloid lycorine, 35 C1,C2-ether analogues of this natural product were synthesized. The compounds were evaluated for antiproliferative activities in vitro in a panel of tumor cell lines with varied levels of apoptosis resistance. A strong correlation between the compound lipophilicity and anticancer activity was observed, indicating that cell permeability properties must be an important determinant in the design of lycorine-based anticancer agents. A theoretical docking model, consistent with the experimental observations, is presented. |