KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Archive for October 9th, 2006

Along came a J. Med. Chem.

Posted by kinasepro on October 9, 2006

Hello KinaseFans,

So what came upon the Kinasepro to rouse him from his slumber was a J. Med. Chem. like a French Roast in the morning.

You see , I’ve inadvertantly attributed the novelty of accessing the ribose binding region off of the quinazoline 5 position to BMS (here and here). For Shame! AstraZeneca in France has quite clearly been at this for a while, and in ASAP today they’ve reported a fair amount about their SRC / ABL candidate: AZD0530.

CN(CC1)CCN1CCOC2=CC(N=CN=C3NC4=C(Cl)C=CC5=C4OCO5)=C3C(OC6CCOCC6)=C2

Some other literature that KP has been oblivious of till now:

BMCL 2006, 1633; MCL 2005, 4226
Process route to AZD0530: WO2006064217

US20060258642
WO2004098604
WO2004087120
WO2004043472
WO2004004732
WO2003045395
WO2003040109
WO2003040108
WO2001094341

The PDB coordinates for the compound are up: 2H8H but they haven’t been released yet. Probably in a few days. From the graphics in JMC 1) the binding mode is as expected, and 2) they need to start using Pymol, because their graphics leave a lot to be desired!

az

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Posted in Astra, bcr abl, SRC | 1 Comment »