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Title: Synthesis and Structure-Activity Relationship of Griseofulvin Analogues as Inhibitors of Centrosomal Clustering in Cancer Cells
Type: Journal articleJournal article
Participant(s):
Author:  Rønnest, Mads Holger (Cwisno: 16330)
Technical University of Denmark

Author:  Rebacz, Blanka (Cwisno: 44720)
Technical University of Denmark

Forfatter:  Markworth, Lene
Technical University of Denmark

Forfatter:  Terp, Anette Hinsch
Technical University of Denmark

Author:  Larsen, Thomas Ostenfeld (Cwisno: 1435)
Technical University of Denmark
Email:

Forfatter:  Krämer, A.
Technical University of Denmark

Author:  Clausen, Mads Hartvig (Cwisno: 6337)
Technical University of Denmark
Email:

Abstract: Griseofulvin was identified as an inhibitor of centrosomal clustering in a recently developed assay. Centrosomal clustering is an important cellular event that enables bipolar mitosis for cancer cell lines harboring supernumerary centrosomes. We report herein the synthesis and SAR of 34 griseofulvin analogues as inhibitors of centrosomal clustering. The variations in the griseofulvin structure cover five positions, namely the 4, 5, 2', 3', and 4' positions. Modification of the 4 and 5 positions affords inactive molecules. The enol ether must be at the 2' position, and the 4' position needs to be Sp2 hybridized. The most active analogues were the 2'-benzyloxy and 2'-(4-methylbenzyloxy) analogues as well as the oxime of the former with a 25-fold increase of activity compared to griscofulvin. Comparison of the results obtained in this work with prior reported growth inhibition data for dermatophytic fungi showed both similarities and differences.
Published: in journal: Journal of Medicinal Chemistry (ISSN: 0022-2623) (DOI: http://dx.doi.org/10.1021/jm801517j), vol: 52, issue: 10, pages: 3342-3347, 2009
DOI:
See the publication in DTU Orbit See the publication in DTU Orbit

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