2j50: Difference between revisions

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==Overview==
==Overview==
The optimization of a series of 5-phenylacetyl, 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives toward the inhibition, of Aurora kinases led to the identification of compound 9d. This is a, potent inhibitor of Aurora kinases that also shows low nanomolar potency, against additional anticancer kinase targets. Based on its high, antiproliferative activity on different cancer cell lines, favorable, chemico-physical and pharmacokinetic properties, and high efficacy in in, vivo tumor models, compound 9d was ultimately selected for further, development.
The optimization of a series of 5-phenylacetyl 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives toward the inhibition of Aurora kinases led to the identification of compound 9d. This is a potent inhibitor of Aurora kinases that also shows low nanomolar potency against additional anticancer kinase targets. Based on its high antiproliferative activity on different cancer cell lines, favorable chemico-physical and pharmacokinetic properties, and high efficacy in in vivo tumor models, compound 9d was ultimately selected for further development.


==Disease==
==Disease==
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[[Category: Berta, D.]]
[[Category: Berta, D.]]
[[Category: Bindi, S.]]
[[Category: Bindi, S.]]
[[Category: Cameron, A.D.]]
[[Category: Cameron, A D.]]
[[Category: Fancelli, D.]]
[[Category: Fancelli, D.]]
[[Category: Forte, B.]]
[[Category: Forte, B.]]
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[[Category: transferase]]
[[Category: transferase]]


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