European Journal of Medicinal Chemistry p. 22 - 32 (2012)
Update date:2022-08-04
Topics:
Rasolofonjatovo, Evelia
Provot, Olivier
Hamze, Abdallah
Rodrigo, Jordi
Bignon, Jérome
Wdzieczak-Bakala, Joanna
Desravines, Déborah
Dubois, Jo?lle
Brion, Jean-Daniel
Alami, Mouad
A novel series of dihydronaphtalene, tetrahydronaphtalene and naphtalene derivatives as restricted analogues of isoCA-4 were designed, synthesized and evaluated for their anticancer properties. High cell growth inhibition against four tumour cell lines was observed at a nanomolar level with dihydronaphtalenes 1d, e and 1h, tetrahydronaphtalene 2c and naphtalene 3c. Structure-activity relationships are also considered. These compounds exhibited a significant inhibitory activity toward tubulin polymerization (IC50 = 2-3 μM), comparable to that of isoCA-4. The effect of the lead compounds 1e and 2c on the cancer cells tested was associated with cell cycle arrest in the G 2/M phase. Docking studies reveal that these compounds showed a binding mode similar to those observed with their non-constraint isoCA-4 and isoerianin congeners.
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Doi:10.1007/BF00921721
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