KinasePro

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

Millennium’s Aurora Compounds

Posted by kinasepro on June 12, 2007

So Millennium is advancing MLN-8237 to phase one, but if the structure I have for MLN-8054 is correct:

O=C(O)C1=CC=C(NC2=NC=C3CN=C(C4=C(F)C=CC=C4F)C5=CC(Cl)=CC=C5C3=N2)C=C1

… then I’m crossing my fingers that MLN-8237 isn’t the methyl ester! All I can find is: US/2005/0256102.

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4 Responses to “Millennium’s Aurora Compounds”

  1. Presume that the carboxylate points out towards solvent and helps solubilise. Often cations are seen doing this; how common is it to see anions in this situation?

  2. kinasepro said

    In a candidate? Not very. Thats why I question I have the right structure =/ It’s usually something you’ll find as a hit and then op-out. If that really is the structure of 8054, then I’d hope it’s doing more then just wafting out in an aqueous breeze.

  3. Maybe they needed it to overcome some hERG inhibition?

  4. Petros said

    The ASCO abstract (Journal of Clinical Oncology, 2007 ASCO Annual Meeting Proceedings Part I. Vol 25, No. 18S (June 20 Supplement), 2007: 3577) highlights the sedative effects seen with this compound, due to its BZD activity!. This necessitated trying qid dosing to mimize the effects.

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