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]
- 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