Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

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Yue EW, DiMeo SV, Higley CA, Markwalder JA, Burton CR, Benfield PA, Grafstrom RH, Cox S, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Trainor GL, Seitz SP

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):343-6.

PubMed ID

14698155 [ View in PubMed

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Abstract

New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains cell culture activity even in the presence of human serum proteins. The most advanced compound did not kill the normal fibroblast line AG1523.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1-(3-(2,4-DIMETHYLTHIAZOL-5-YL)-4-OXO-2,4-DIHYDROINDENO[1,2-C]PYRAZOL-5-YL)-3-(4-METHYLPIPERAZIN-1-YL)UREA	Cyclin-dependent kinase 2	IC 50 (nM)	8	7.6	22	Details