5-Substituted [1]pyrindine derivatives with antiproliferative activity.
We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but have interestingly no effect against the normal human fibroblasts CRL-2796. Generally, these pyrindines are active on both tumor cell lines. Compounds bearing large substituents with structural rigidity at position 5 such as phenyl-furyl show no inhibition of cell growth.
Kolb
Stéphanie
S
Laboratoire de Pharmacochimie Moléculaire et Cellulaire, Université Paris Descartes, UFR Biomédicale, 45 rue des Saints-Pères, Paris, F-75006, France; INSERM U648, Paris F-75006, France.
Goddard
Mary-Lorène
ML
Loukaci
Ali
A
Mondésert
Odile
O
Ducommun
Bernard
B
Braud
Emmanuelle
E
Garbay
Christiane
C
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005347:Fibroblasts / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry*
D000970:Antineoplastic Agents; D011725:Pyridines