Synthesis and antitumor activity of amine analogs of irofulven

Acylfulvenes, a class of semisynthetic analogs of Illudin S, show high toxicity toward prostate cancer cells. Here we probe the effect of changes in hydrophilic character of the analogs.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-12, Vol.17 (24), p.6770-6772
Main Authors: McMorris, Trevor C., Chimmani, Ramesh, Gurram, Mahender, Staake, Michael D., Kelner, Michael J.
Format: Article
Language:English
Subjects:
Adenocarcinoma - pathology
Amines - chemistry
Analogs synthesis
Antineoplastic agents
Antineoplastic Agents, Alkylating - chemical synthesis
Antineoplastic Agents, Alkylating - chemistry
Antineoplastic Agents, Alkylating - toxicity
Antitumor activity
Biological and medical sciences
Cell Line, Tumor
Cell Survival - drug effects
General aspects
Humans
Inhibitory Concentration 50
Irofulven
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Reductive amination
Sesquiterpenes - chemical synthesis
Sesquiterpenes - chemistry
Sesquiterpenes - toxicity
Staudinger ligation
Structure-Activity Relationship
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Description
Summary:Acylfulvenes, a class of semisynthetic analogs of Illudin S, show high toxicity toward prostate cancer cells. Here we probe the effect of changes in hydrophilic character of the analogs.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.10.040