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


Posted by kinasepro on October 24, 2006

How now Schering-Plough, Nice purvalanol analogs as CDK2 inhibitors.

Anything earthshaking here? Hmm… Not really, but look hard enough, and KP always learns something.

Yep, hadn’t noticed the bromide as an isopropyl isostere before, but this is a continuation from US2006041131, WO2004022559. Schering has been beating on this and other 6-5 purine isosteres for some time (WO2004026877). There’s been plenty of Biotech sniffing around here. Vernalis has a similar CDK series (WO2004087707), and a Bioorg. Med. Chem. Lett. 2005, 863 (appears they’ve dropped the series).  Ono has some c-Jun (WO2005035516) inhibitors on the scafford. So whats new here? Vernalis describes selectivity issues.  Maybe they cracked that nut, otherwise its not obvious to me.
BrC2=C1N(N=C2)C(NC3=CC=NC=C3)=CC(C4CCCNC4)=N1 BrC2=C1N(N=C2)C(NC3=CC=CN=C3)=CC(N4CCC[C@@H]4CO)=N1 CC(C)N2C=NC1=C(NC3=CC(Cl)=CC=C3)N=C(N[C@H]([C@H](C)C)CO)N=C12


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