3LGP

Structure and activity relationships of tartrate-based TACE inhibitors.

Li, D., Popovici-Muller, J., Belanger, D.B., Caldwell, J., Dai, C., David, M., Girijavallabhan, V.M., Lavey, B.J., Lee, J.F., Liu, Z., Mazzola, R., Rizvi, R., Rosner, K.E., Shankar, B., Spitler, J., Ting, P.C., Vaccaro, H., Yu, W., Zhou, G., Zhu, Z., Niu, X., Sun, J., Guo, Z., Orth, P., Chen, S., Kozlowski, J.A., Lundell, D.J., Madison, V., McKittrick, B., Piwinski, J.J., Shih, N.Y., Shipps, G.W., Siddiqui, M.A., Strickland, C.O.

(2010) Bioorg Med Chem Lett 20: 4812-4815

• PubMed: 20638281 Search on PubMed
• DOI: https://doi.org/10.1016/j.bmcl.2010.06.104
• Primary Citation of Related Structures:  
  3LGP


• PubMed Abstract: 
  

  The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokinetics.

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Organizational Affiliation: 

Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, 320 Bent Street, Cambridge, MA 02141, United States. dansu.li@spcorp.com