Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.

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Trova MP, Barnes KD, Alicea L, Benanti T, Bielaska M, Bilotta J, Bliss B, Duong TN, Haydar S, Herr RJ, Hui Y, Johnson M, Lehman JM, Peace D, Rainka M, Snider P, Salamone S, Tregay S, Zheng X, Friedrich TD

Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6613-7. doi: 10.1016/j.bmcl.2009.10.011. Epub 2009 Oct 12.

PubMed ID
19854650 [ View in PubMed
]
Abstract

C-6 Biarylmethylamino purine derivatives of roscovitine (1) inhibit cyclin dependent kinases and demonstrate potent antiproliferative activity. Replacement of the aryl rings of the C-6 biarylmethylamino group with heterobiaryl rings has provided compounds with significantly improved activity. In particular, derivatives 18 g and 9 c demonstrated 1000-fold and 1250-fold improvements, respectively, in the growth inhibition of HeLa cells compared to roscovitine (1).

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SeliciclibCyclin-dependent kinase 2IC 50 (nM)4600N/AN/ADetails
SeliciclibCyclin-dependent kinase 2IC 50 (nM)520N/AN/ADetails