KinasePro

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

Some highlights…

Posted by kinasepro on November 28, 2007

GSK’s been looking at Plk1 for quite a while. Sure the structure was in an earlier application (March), but here it is better late then never. See: WO/2004/074244, WO/2004/087652, WO/2005/019193, WO/2007/030361, US20070010668, & US20070270437

AP-24534 In here? Earlier Ariad had a double bond wiggling around T315I, in WO/2007/133560 & WO/2007/133562 it’s a triple bond.

And Vertex has an interesting series of series of Rock inhibitors in WO/2007/133622. Ki is reported to be <100 nM and clean across the cyps.

Oh yah, and if your curious about Cyclacel’s Aurora inhibitor CYC-116, they’ve narrowed it down to 1 of 3 for you and they also give an in vitro panel in WO/2007/132220, WO/2007/132221, WO/2007/132228. The claims make it look like the morpholine.

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4 Responses to “Some highlights…”

  1. Is the thiophene really necessary or do they just enjoy the thrill of reactive-metabolite roulette?

  2. kinasepro said

    Nah, thiazoles’r fine too

  3. weirdo said

    Funny, I focused in on the fluoropyridine in the Vertex molecule myself . . .

  4. milkshake said

    There is nothing wrong with thiophenes – only with the people who put them in the drugs (just kidding) . It is interesting that you mentioned the possibility of reactive metabolite of thiophene because we have a DMPK man who used to work on the BMS aminothiazole Src-Abl compound and apparently they were very worried about the reactive metabolites they saw happening on the aminothiazole. ut it was no show-stopper in the end. I guess electrophilic metabolites are more permissible, with anti-cancer compounds…

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