Treatment of cancer using organoarsenicals
AssigneeThe Florida International University Board of Trustees
InventorsBarry P. ROSEN, Kunie YOSHINAGA-SAKURAI, Venkadesh Sarkarai NADAR
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Abstract
The subject invention provides organoarsenicals or salts thereof, compositions comprising an organoarsenical or a salt thereof, and methods of using the organoarsenicals or salts thereof, or compositions for inhibiting glutaminase and for treating cancers. Specifically, the subject invention provides methods of inhibiting glutaminase (e.g., KGA) catalytic activity in a cell, methods of treating cancer or a tumor via, for example, the inhibition of glutaminase activity, and methods of disrupting and/or inhibiting growth and proliferation of cancerous or tumorous cells.
Claims20
A composition comprising a trivalent organoarsenical, a pentavalent organoarsenical, or a salt thereof, and a pharmaceutically-acceptable carrier.
A method of inhibiting glutaminase activity in a cell, comprising contacting the cell with a trivalent organoarsenical, a pentavalent organoarsenical, or a salt thereof.
A method of disrupting and/or inhibiting growth and proliferation of cancerous or tumorous cells, the method comprising introducing into an environment in which the cancerous or tumorous cells exist, an effective amount of a trivalent organoarsenical, a pentavalent organoarsenical, or a salt thereof, the pentavalent organoarsenical having a general structure of formula (I):
- wherein Z is OR7, NHR8, NR8R9 or NHCHR10R11;
- R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are independently selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, benzyl, substituted benzyl, benzoyl, substituted benzoyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, substituted alkenyl, alkynyl, alkoxy, substituted alkoxy, acyl, sulfhydryl, halogen, amino, substituted amino, hydroxyl, hydroxylalkyl, substituted hydroxylalkyl, —C(O)R12, —COOR13, and —OR14, and
- R12, R13 and R14 are independently selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, benzyl, substituted benzyl, benzoyl, substituted benzoyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, substituted alkenyl, alkynyl, alkoxy, substituted alkoxy, acyl, sulfhydryl, halogen, amino, substituted amino, hydroxyl, hydroxylalkyl, and substituted hydroxylalkyl.
Dependencies are inferred from the claim text.