hTERT modulators and methods of use
AssigneeArizona Board of Regents
InventorsLaurence Hurley, Vijay Gokhale, HyunJin Kang, Kui Wu
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Abstract
The present invention provides hTERT modulators and methods for producing and using the same. In particular, the present invention provide a compound of the formula as described herein. Some aspects of the invention are based on the characterization of the effect of hTERT core promoter region mutants on the 5-12 G-quadruplex structure and its stability. It is believed that some of the compounds of the invention bind selectively to the G-quadruplex in the hTERT core promoter mutant, which results in reversal of the effect of mutant promoter activation.
Claims11
A compound selected from the group consisting of:
- 2-amino-N-((4-methoxy-3-methylphenyl)carbamoyl)benzamide,
- 2-amino-N-((4-((2-chloropyrimidin-5-yl)oxy)-3-methylphenyl)-carbamoyl)benzamide,
- 2-amino-N-((3-methyl-4-(pyrazine-2-yloxy)phenyl)carbamoyl)-benzamide,
- 2-amino-N-((3-methyl-4-((5-(trifluoromethyl)pyrimidin-2-yl)oxy)phenyl)carbamoyl)benzamide,
- 2-amino-N-((4-((5-methoxypyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)benzamide,
- N-((4-((5-bromopyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)-4-(trifluoromethyl)benzamide,
- N-((4-((5-bromopyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)-4-fluorobenzamide,
- N-((4-((5-bromopyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)-4-methoxybenzamide,
- 2-amino-N-((4-(2-morpholinoethoxy)phenyl)carbamoyl)benzamide,
- 2-amino-N-((4-((5-(1-methyl-1H-pyrazol-4-yl)pyrimidin-2-yl)oxy)phenyl)carbamoyl)benzamide,
- N-((4-((5-bromopyrimidin-2-yl)oxy)phenyl)carbamoyl)-4-methoxybenzamide,
- N-((3-chloro-4-((5-chloropyrimidin-2-yl)oxy)phenyl)carbamoyl)-4-methoxybenzamide,
- 4-methoxy-N-((3-methyl-4-((5-(1-methyl-1H-pyrazol-4-yl)pyrimidin-2-yl)oxy)phenyl)carbamoyl)benzamide,
- N-((4-((5-bromopyrimidin-2-yl)oxy)phenyl)(methyl)carbamoyl)-4-methoxybenzamide,
- N-((4-((5-bromopyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)picolinamide,
- N-((4-guanidino-3-methylphenyl)carbamoyl)benzamide,
- N-((4((5-chloropyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)-4-(trifluoromethyl)benzamide,
- N-((4((5-methoxypyrimidin-2-yl)oxy)-3-methylphenyl)carbamoyl)-4-(trifluoromethyl)benzamide,
- N-((4-((5-chloropyrimidin-2-yl)oxy)-3-fluorophenyl)carbamoyl)-4-(trifluoromethyl)benzamide,
- N-((3-methyl-4-(pyrazin-2-yloxy)phenyl)-carbamoyl)-4-(trifluoromethyl)benzamide, and
- N-((4-((2-chloropyrimidin-5-yl)oxy)-3-methylphenyl)carbamoyl)-4-(trifluoromethyl)benzamide,
- including a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a mixture thereof.
Dependencies are inferred from the claim text.