Compounds that abrogate dna damage induced cell cycle g2 checkpoint and/or augment anti-cancer activity of dna-damaging treatments
AssigneeCanBas Co., Ltd.
InventorsTAKUMI KAWABE, Hidetaka Kobayashi
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Abstract
The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.
Claims32
1-50. (canceled)
An ex vivo method for suppressing or killing a DNA-damaged cell, comprising administering an effective amount of at least one compound that abrogates the cell cycle G2 checkpoint when administered to a cell, wherein the compound has the following structure:
- where either or both of benzene can be substituted with pyrazine, pyrimidine piperazine, morpholine, cyclohexane, piperizine or pyridine;
- R1 is a halogen, bromine (Br), chlorine (Cl), fluorine (F), iodine (I), amino (NH2), nitro (NO2), hydroxy (OH), O-methyl (OCH3), methyl (CH3) or hydrogen (H);
- R2, R3, R4, R5 and R6 is bromine (Br), chlorine (Cl), fluorine (F), iodine (I), amino (NH2), nitro (NO2), methyl (CH3), O-methyl (OCH3), hydroxy (OH), CH(CH3)2, CHO, CHOCH3, O(CH2)nCH3, OCO(C6H12)Cl, COOCH3 or hydrogen;
- X1 is nitrogen (NH), oxygen (O) or sulfate (S);
- and X2 is oxygen (O) or sulfate (S).
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Dependencies are inferred from the claim text.