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 suitable tools for affinity studies directed to find additional intracellular paullone targets.
Universität Hamburg, Institut für Pharmazie, Bundesstrasse 45, Germany.
Karen
K
Wieking
Marie
M
Knockaert
Maryse
M
Leost
Daniel W
DW
Zaharevitz
Laurent
L
Meijer
Conrad
C
Kunick
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001552:Benzazepines; D004791:Enzyme Inhibitors; D016203:CDC2 Protein Kinase