Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.

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Lee J, Choi H, Kim KH, Jeong S, Park JW, Baek CS, Lee SH

Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2292-5. doi: 10.1016/j.bmcl.2008.03.002. Epub 2008 Mar 6.

PubMed ID

18353638 [ View in PubMed

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Abstract

A novel series of 3,5-diaminoindazoles were prepared and found to be CDK inhibitors. Potent inhibitors against CDK1 and CDK2 were obtained by introduction of 1lambda(6)-isothiazolidine-1,1-dioxide at 5-position of indazole. Anti-proliferative activities of compounds were evaluated using EJ, HCT116, SW620, and A549 cancer cell lines.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
N-[5-(1,1-DIOXIDOISOTHIAZOLIDIN-2-YL)-1H-INDAZOL-3-YL]-2-(4-PIPERIDIN-1-YLPHENYL)ACETAMIDE	Cyclin-dependent kinase 2	IC 50 (nM)	30	N/A	N/A	Details