title: Synthesis and antitumor characterization of pyrazolic analogues of the marine pyrroloquinoline alkaloids: wakayin and tsitsikammamines.
abstract: A series of aza analogues of the marine alkaloids wakayin and tsitsikammamines A and B have been synthesized. The strategy used was based on [3 + 2] cycloaddition reactions involving 3-ethylamine-indole-4,7-dione and different diazo reagents. All the compounds were evaluated in vitro for antiproliferative activity against five distinct cancer cell lines and for their inhibitory effect on topoisomerase isoenzymes I and II. Some of the compounds inhibited the topoisomerase I and/or II catalyzed relaxation of supercoiled DNA at a concentration comparable to the drugs camptothecin and etoposide. Only a few of them exhibited cytotoxic activity with IC50 values in the micromolar range.
authors: Laboratoire SPCMIB, UMR-CNRS 5068, Université Paul Sabatier, 118 route de Narbonne, 31062, Toulouse Cedex 4, France.
authors: Laurent
authors: L
authors: Legentil
authors: Laurent
authors: L
authors: Benel
authors: Viviane
authors: V
authors: Bertrand
authors: Brigitte
authors: B
authors: Lesur
authors: Evelyne
authors: E
authors: Delfourne