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Paper | Special issue | Vol 90, No. 1, 2015, pp.316-326
Published online, 7th May, 2014
DOI: 10.3987/COM-14-S(K)20
Bisindole Alkaloids Condensed with a Cyclopropane Ring, Part 2. Cyclopropano-vinorelbine and Its Derivatives

Péter Keglevich, László Hazai, Zsófia Dubrovay, Zsuzsanna Sánta, Miklós Dékány, Csaba Szántay, Jr., György Kalaus, and Csaba Szántay*

*Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, H-1111 Budapest, Szt. Gellért tér 4, Hungary

Abstract

Vinorelbine condensed with a cyclopropane ring in the position 14 and 15 of the vindoline monomer part was synthesized and was found to have excellent antitumor activity. Further derivatives of cyclopropano-vinorelbine were prepared, the vincristine-like derivative, the N1-formyl-cyclopropano-vinorelbine, and the hydrated vinorelbine analogue, i.e. 5’-desmethylene-cyclopropano-vinblastine.