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Chemical Structure Hypocretins

alsterpaullone gwennpaullone

Fig. 4 Chemical structure of the most frequently used paullones. The description of their synthesis has been described in detail: paullone (Kunick 1992), kenpaullone (Kunick 1992; Schultz et al. 1999), alsterpaullone (Schultz et al. 1999), gwennpaullone (Wieking et al. 2002)

o alsterpaullone gwennpaullone

Fig. 4 Chemical structure of the most frequently used paullones. The description of their synthesis has been described in detail: paullone (Kunick 1992), kenpaullone (Kunick 1992; Schultz et al. 1999), alsterpaullone (Schultz et al. 1999), gwennpaullone (Wieking et al. 2002)

PARE with the CDK inhibitor flavopiridol (NSC-649890) as a reference to identify compounds in the NCI collection that might act through CDK inhibition (Zaharevitz 1999). The highest COMPARE correlation coeffi-cient (0.67) was found to be with another CDK inhibitor, olomoucine (NSC-666096) (Vesely et al. 1994). Among five other compounds displaying a correlation coefficient with flavopiridol superior to 0.60, one compound (NSC-664704) was by far the most active against CDK1/cyclin B (IC50: 0.4 mM). This benzazepinone, 9-bromo-7,12-dihydro-indolo[3,2-d]benzazepin-6(5H)-one (Fig. 4), had been synthesised earlier by one of us (Kunick 1992). We renamed it kenpaullone to honour the memory of Dr. Kenneth Paull. Paullone was the name given to the unsubstituted ring structure.

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