Cytotoxic Michael-type amine adducts of alpha-methylene lactones alantolactone and isoalantolactone

Authors
Lawrence, NJ McGown, AT Nduka, J Hadfield, JA Pritchard, RG
Citation
Nj. Lawrence et al., Cytotoxic Michael-type amine adducts of alpha-methylene lactones alantolactone and isoalantolactone, BIOORG MED, 11(3), 2001, pp. 429-431
Citations number
28
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
429 - 431
Database
ISI
SICI code
0960-894X(20010212)11:3<429:CMAAOA>2.0.ZU;2-Y
Abstract
Two series of cytotoxic (IC50, K562 cell line, 1-24 muM) alpha -aminomethyl substituted lactones 3 and 4 were prepared by stereoselective Michael-type addition of amines to alantolactone (1) and isoalantolactone (2). The lact ones 1 and 2 and their amine adducts induce apoptosis and act as alkylating agents. (C) 2001 Elsevier Science Ltd. All rights reserved.