Synthesis and cytotoxicity of 28-n-propargylaminoalkylated 2,3-indolotriterpenic acids

Abstract

A new series of propargylaminoalkyl derivatives with N-methylpiperazine and morpholine fragments was obtained by modification of the carboxyl group of [3,2b]-indolotriterpenic acids (N-propargylation, Cu(I) catalyzed Mannich reaction). Cytotoxicity assays demonstrated that oleanane-type conjugate with N-methylpiperazine exhibited high antitumor activity against leukemia cell line SR and non-small cell lung cancer cell line NCI-H460.