Download MendeleyDesign, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Zhang, L., Fan, J., Chong, J.H., Cesena, A., Tam, B.Y., Gilson, C., Boykin, C., Wang, D., Aivazian, D., Marcotte, D., Xiao, G., Le Brazidec, J.Y., Piao, J., Lundgren, K., Hong, K., Vu, K., Nguyen, K., Gan, L.S., Silvian, L., Ling, L., Teng, M., Reff, M., Takeda, N., Timple, N., Wang, Q., Morena, R., Khan, S., Zhao, S., Li, T., Lee, W.C., Taveras, A.G., Chao, J.(2011) Bioorg Med Chem Lett 21: 5633-5637
- PubMed: 21798738
- DOI: https://doi.org/10.1016/j.bmcl.2011.06.129
- Primary Citation of Related Structures:
3R21, 3R22 - PubMed Abstract:
A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1). These inhibitors were originally designed based on an early lead (compound I). SAR development has led to the discovery of potent inhibitors with single digit nM IC(50)s towards both AKA and CDK1. An exemplary compound 1a has demonstrated good efficacy in an HCT116 colon cancer xenograft model.
Organizational Affiliation:
Biogen Idec, 5200 Research Place, San Diego, CA 92122, United States. lin.zhang.ge@sbcglobal.net
