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Bioorg Med Chem Lett. 2016 Apr 1;26(7):1836-8. doi: 10.1016/j.bmcl.2016.02.028. Epub 2016 Feb 13.

Hydroxyurea derivatives of irofulven with improved antitumor efficacy.

Author information

1
Department of Chemistry & Biochemistry, University of California, San Diego, La Jolla, CA 92093-0358, USA.
2
Department of Pathology, University of California, San Diego, MC 7721, La Jolla, CA 92093-7721, USA.
3
Department of Pathology, University of California, San Diego, MC 7721, La Jolla, CA 92093-7721, USA. Electronic address: mkelner@ucsd.edu.

Abstract

Irofulven is a semi-synthetic derivative of Illudin S, a toxic sesquiterpene isolated from the mushroom Omphalotus illudens. Irofulven has displayed significant antitumor activity in various clinical trials but displayed a limited therapeutic index. A new derivative of irofulven was prepared by reacting hydroxyurea with irofulven under acidic conditions. Acetylation of this new compound with acetic anhydride produced a second derivative. Both of these new derivatives displayed significant antitumor activity in vitro and in vivo comparable to or exceeding that of irofulven.

KEYWORDS:

Analog LP-184; Hydroxyurea; Illudin S; Irofulven; Xenograft

PMID:
26922141
DOI:
10.1016/j.bmcl.2016.02.028
[Indexed for MEDLINE]

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