ChemInform Abstract: Inhibition of Tubulin Polymerization by 5,6‐Dihydroindolo[2,1‐a]isoquinoline Derivatives.

Abstract

Inhibition of Tubulin Polymerization by 5,6-Dihydroindolo[2,1a]isoquinoline Derivatives. -3-Hydroxy-substituted indoloisoquinolines, e.g. (I), as well as their corresponding methyl ethers, both series exhibiting cytostatic activity, are evaluated for inhibition of tubulin polymerization. Only in case of the hydroxy series correlation between inhibition of tubulin polymerization and cytostatic activity is established, whereas the methyl ether series act certainly via an alternate mechanism. The (+)-enantiomers of compounds (Ia) and (Ib) show the highest activity as inhibitors of tubulin polymerization. -(GOLDBRUNNER, M.; LOIDL, G.; POLOSSEK, T.; MANNSCHRECK, A.; VON ANGERER, E.; J. Med. Chem. 40 (1997) 22, 3524-3533; Inst. Pharm., Univ. Regensburg, D-93053 Regensburg, Germany; EN)