Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.

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Pinkerton AB, Lee TT, Hoffman TZ, Wang Y, Kahraman M, Cook TG, Severance D, Gahman TC, Noble SA, Shiau AK, Davis RL

Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3562-9. doi: 10.1016/j.bmcl.2007.04.076. Epub 2007 Apr 29.

PubMed ID

17498954 [ View in PubMed

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Abstract

We have identified and synthesized a series of thiophene containing inhibitors of kinesin spindle protein. SAR studies led to the synthesis of 33, which was co-crystallized with KSP and determined to bind to an allosteric pocket previously described for other known KSP inhibitors.