Synthesis of Paullones with Aminoalkyl Side Chains

Paullones 3 and 4 with aminoalkyl side chains in 2‐ or 3‐position were synthesized as derivatives of kenpaullone 1. Both 3 and 4 showed the characteristic CDK1‐inhibitory activity of the paullones and a modest antiproliferative activity on cultured human tumor cell lines. Hence, 3 and 4 appear to be...

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Bibliographic Details
Published in:Archiv der Pharmazie (Weinheim) 2002-07, Vol.335 (7), p.311-317
Main Authors: Wieking, Karen, Knockaert, Marie, Leost, Maryse, Zaharevitz, Daniel W., Meijer, Laurent, Kunick, Conrad
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antitumor activity
Benzazepines - chemical synthesis
Benzazepines - chemistry
Benzazepines - pharmacology
Benzazepinones
Biological and medical sciences
CDC2 Protein Kinase - antagonists & inhibitors
Cyclin-dependent kinases
Drug Screening Assays, Antitumor
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
Humans
Inhibitors
Medical sciences
Molecular Structure
Paullones
Pharmacology. Drug treatments
Tumor Cells, Cultured
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Summary:Paullones 3 and 4 with aminoalkyl side chains in 2‐ or 3‐position were synthesized as derivatives of kenpaullone 1. Both 3 and 4 showed the characteristic CDK1‐inhibitory activity of the paullones and a modest antiproliferative activity on cultured human tumor cell lines. Hence, 3 and 4 appear to be suitable tools for affinity studies directed to find additional intracellular paullone targets.
ISSN:0365-6233
1521-4184
DOI:10.1002/1521-4184(200209)335:7<311::AID-ARDP311>3.0.CO;2-F