Novel carboxylesterase inhibitors (SJ-02-0030)

St. Jude Reference #SJ-02-0030


Novel classes of compounds which have useful carboxylesterase inhibitory activity are provided, including both generic inhibitors, as well as compounds selective for the human intestinal carboxylesterase. These compounds can be used to treat or ameliorate the toxic effects of cancer therapy drugs (such as CPT-11), the effects of the drug overdose, or to increase the efficacy of existing insecticides and pesticides.


carboxylesterase inhibitors

Granted patents or published Applications

US 7,973,034

Related scientific references

Wadkins, R.M. et al., "Discovery of Novel Selective Inhibitors of Human Intestinal Carboxylesterase for the Amelioration of Irinotecan-Induced Diarrhea:  Synthesis, Quantitative Structure-Activity Relationship Analysis, and Biological Activity." Molecular Pharmacology 65(6): 1336-1342 (June 2004);

Wadkins R.M., et al., "Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases." Journal of Medicinal Chemistry 48:2906-2915, 2005.

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