ChemInform Abstract: Synthesis of Indolizidinone Analogues of Cytotoxic Alkaloids: Monocyclic Precursors Are also Active.

Abstract

Synthesis of Indolizidinone Analogues of Cytotoxic Alkaloids: Monocyclic PrecursorsAre also Active. -A two-step route is reported for the transformation of readily available hydroxyproline N-amides into indolizidinone derivatives of type (V) and (VI). The cytotoxic activity of the compounds is studied against the human neuroblastoma SHSY-5Y and human breast cancer MCF-7 cell lines. Especially the derivatives with the bulky biphenyl substituent (Vb) or (VIb) display cytotoxic activities at 30 μM for 48 h. The monocyclic precursors of type (VII) show a comparable or higher cytotoxicity than the bicyclic derivatives. -(BOTO*, A.; MIGUELEZ, J.; MARIN, R.; DIAZ, M.; Bioorg. Med. Chem. Lett. 22 (2012) 10, 3402-3407, http://dx.