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


Posted by kinasepro on December 10, 2006

G’day Kinacia (formerly Thrombogenix) I see you guys made a splash with TGX-221, a selective Pi3K-b inhibitor. And now it looks like you’ve been fine tuneing. I’m thinking the Bioorg Med Chem Lett will look something like:

LY294002 is: 1E7V

221: WO/2001053266

6 Responses to “US20060276470”

  1. Think they used to be called Cerylid too?

    Are these bad boys irreversible inhibitors? – rather nice beta-keto-enamine in the LY compound looking like its gagging for a nucleophile there, although that has been deactivated some in these new compounds.

  2. milkshake said

    these are not irreversible inhibitors most likely – but the morpholino-chromones do have a stability problem especialy in basic conditions. I like the chromone isoster they came up with.

  3. kinasepro said

    1E7V shows you how they bind… The morpholine oxygen behaves as the hinge hydrogen bond acceptor, but since you mention it… It surprised me to learn that scifinder is teeming with compounds bearing the pyridopyrimidinone core.

  4. milkshake said

    I did not know this. It explains why replacing morpholine with piperidine in closely-related 2-(N-morpholinyl)-pyrone series obliterates the activity.

  5. kinasepro said

    As you might expect the 4-pyridines are well staked out in the above exemplified series…

  6. kinasepro said

    KP is a little slower on the uptick then your average bear.

    So here’s a belated link to a related compound:

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