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Archive for the ‘Plk1’ Category

BI-6727

Posted by kinasepro on May 12, 2009

BI’s PhII follow on to BI-2536

O=C(N[C@H]1CC[C@H](N2CCN(CC3CC3)CC2)CC1)C4=CC=C(NC(N=C5N(C(C)C)[C@@H]6CC)=NC=C5N(C)C6=O)C(OC)=C4

PDB: 3FC2; Clin Can Res

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Takeda’s got PLK1

Posted by kinasepro on April 2, 2009

WO/2009/042806 & WO/2009/042711

FC1(F)CN(C2CCCC2)C(N=C3NC(C=CC(C(NC4CCN(CC4)C)=O)=C5)=C5OC)=C(C=N3)N(C)C1=O

process app.

Posted in Plk1, Takeda | 2 Comments »

BI-2536

Posted by kinasepro on April 2, 2009

BI’s Ph2 PLK1 inhibitor

O=C(C1=CC=C(C(OC)=C1)NC2=NC=C(N(C3=O)C)C(N([C@@H]3CC)C4CCCC4)=N2)NC5CCN(CC5)C

IV / 0.8 nM

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ON-01910

Posted by kinasepro on April 2, 2009

Onconova’s IV Ph2 PLK1’inhibitor’

O=S(CC1=CC(NCC(O[Na])=O)=C(OC)C=C1)(/C=C/C2=C(OC)C=C(OC)C=C2OC)=O

…a new chemical entity that arrests cancer cells in G2/M by modulating mitotic regulatory pathways including polo-like kinase 1 (Plk1).” via WO/2008/088803

Posted in Plk1 | 8 Comments »

PDB Update

Posted by kinasepro on October 7, 2008

Buncha-new Plk1 PDB’s

Plk1: 3DBF, 3DBE, 3DBD, 3DBC, 3DB8

new c-Met: 3EFK, 3EFJ

new Vegf: 3CJG, 3CJF

Posted in c-Met, PDB, Plk1, VEGF | Leave a Comment »

R & D @ B I

Posted by kinasepro on September 13, 2008

With BIRB-796 a distant memory, BIBW-2992 in ph3 and given the new name Tovok, BIBF-1120 headed into ph3 and given the name Vargatef,  BI-2536 in multiple Ph2s, a new Ph1 Aurora inhibitor, and another backup PLK1 inhibitor undisclosed, but likely in-clinic or clinic-bound – what could possibly be next?

I can haz pyrimidines

PDK mod prolly from Berlex

Posted in BI, PDK1, PKC, Plk1 | 2 Comments »

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.

Posted in Ariad, bcr abl, Cyclacel, GSK, Plk1, Rho, Vertex | 4 Comments »

BI’s PLK1 compound

Posted by kinasepro on August 19, 2007

WO/2007/90844 is a salt form application of a compound that we’ve seen before ’round here.

O=C(N[C@@H]1CC[C@@H](N2CCN(CC3CC3)CC2)CC1)C4=CC=C(NC(N=C5N(C(C)C)[C@@H]6CC)=NC=C5[N](C)(C)C6=O)C(OC)=C4

discovery: WO/2003/020722, WO/2004/076454

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PDB Update

Posted by kinasepro on April 24, 2007

>> Update >> Biochemistry article on the Plk1 structure.

Woohoo! First published kinase domain Plk1 structures from Pfizer:

2OWB Plk1 w/ pyrrolopyrazole inhibitor
2OU7 Plk1 w/ ANP

and a Chk1 structure from Merck: 2HOG; BMCL

Posted in Chk1, PDB, Plk1 | 4 Comments »

DE102005020104

Posted by kinasepro on October 29, 2006

and DE102005020105. Guten Tag Schering AG,

Further along the road with the thiazolidinones, eh?  I like the title: New thiazolidinone without basic nitrogen, their production and use as drugs

Kinasepro is always happy to see more Plk1 inhibitors, but hey I’ll admit that I haven’t a clue whats going on with these – and now consider an earlier post on your analogous series, ummm, wrong. The only PDBs that give KP a hint as to what could be going on here are from some compounds bound to PI3K: 2A4Z, and 2A5U. O=C(N(CC)/C(S2)=C(C(NCC(F)(F)F)=O)\C#N)/C2=C/C1=C(C)N=CN1 O=C(N(CC)/C(S2)=C(C(NCC#C)=O)\C#N)/C2=C/C1=CC=C(N3CCCC3)C=C1

Posted in Plk1, Schering AG, Uncategorized | Leave a Comment »