Patent Number: 8,716,329

Title: Use of parthenolide derivatives as antileukemic and cytotoxic agents

Abstract: The present invention provides compounds of the formula (I) ##STR00001## wherein: X.sub.1, X.sub.2 and X.sub.3 are heteroatoms; R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are independently selected from H, halo, --OH, --NO.sub.2, --CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C.sub.1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, --CN, --C(O)--, --C(O)C(O)--, --C(O)NR.sup.1--, --C(O)NR.sup.1NR.sup.2--, --C(O)O--, --OC(O)--, --NR.sup.1CO.sub.2--, --O--, --NR.sup.1C(O)NR.sup.2--, --OC(O)NR.sup.1--, --NR.sup.1NR.sup.2--, --NR.sup.1C(O)--, --S--, --SO--, --SO.sub.2--, --NR.sup.1--, --SO.sub.2NR.sup.1--, --NR.sup.1R.sup.2, or --NR.sup.1SO.sub.2--, wherein R.sup.1 and R.sup.2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR.sup.1R.sup.2, R.sup.1 and R.sup.2 optionally together with the nitrogen atom form an optionally substituted 5-12 membered ring, said ring optionally comprising 1 or more heteroatoms or a group selected from --CO--, --SO--, --SO.sub.2-- and --PO--; or a pharmaceutically acceptable salt, ester or prodrug thereof.

Inventors: Crooks; Peter A. (Nicholasville, KY), Jordan; Craig T. (Rochester, NY), Wei; Xiaochen (Lexington, KY)

Assignee: University of Kentucky

International Classification: A61K 31/35 (20060101); C07D 405/00 (20060101); C07D 411/00 (20060101)

Expiration Date: 5/06/12018