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Synthesis and Biological Evaluation of Antitumor‐Active Arglabin Derivatives
Author(s) -
Csuk René,
Heinold Anke,
Siewert Bianka,
Schwarz Stefan,
Barthel Alexander,
Kluge Ralph,
Ströhl Dieter
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201100065
Subject(s) - cytotoxicity , sulforhodamine b , chemistry , double bond , moiety , stereochemistry , methylene , selectivity , chemical synthesis , biological activity , combinatorial chemistry , organic chemistry , in vitro , biochemistry , catalysis
Arglabin derivatives varied at the endo‐ or exo‐cyclic double bond were synthesized and studied in a colorimetric sulforhodamine B assay for their cytotoxicity. Variations on the endocyclic double bond led to compounds of reduced cytotoxicity whereas derivatives from the reaction of the α‐methylene‐γ‐butyrolactone moiety led to compounds of similar or only slightly reduced cytotoxicity but different, cell line‐dependent selectivity. In addition, arglabin is an excellent starting material for the synthesis of the guaianolide arborescin.