Design and preparation of aza-analogues of benzo[c]phenanthridine framework with cytotoxic and antiplasmodial activities.
Benzo[c]phenanthridine alkaloids represent interesting lead for the discovery of new potential antiplasmodial and/or anticancer drugs. In this field, a novel library of aza-analogs of benzo[c]phenanthroline framework derivatives was designed and prepared. Although these compounds did not have specific antiplasmodial activities, some of them displayed specific in vitro activity against two cancer lines especially compound 24 with an IC(50) against the MCF7 line of 0.6 microM.
Yapi
Ange-Désiré
AD
Laboratoire de chimie organique et thérapeutique, EA 3660 Unité de Molécules d'Intérêt Biologique, Faculté de Pharmacie, 7 boulevard Jeanne d'Arc, BP 89700, 21079 Dijon, France.
Desbois
Nicolas
N
Chezal
Jean-Michel
JM
Chavignon
Olivier
O
Teulade
Jean-Claude
JC
Valentin
Alexis
A
Blache
Yves
Y
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001372:Aza Compounds / Q000737:chemistry*; D053119:Benzophenanthridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects*
D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D001372:Aza Compounds; D053119:Benzophenanthridines