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US 2022/0033382 A9Published application
Prodigiosin Analogs And Methods Of Use
AssigneeInstitute for Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center
InventorsWafik S. El-Deiry, Xiaobing Tian
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Abstract
Prodigiosin analogs which reactivate the p53 pathway are provided, as well as compositions of these compounds, and methods for reactivation of the p53 pathway using these compounds are provided. The prodigiosin analogs may be used to treat cancer in which p53 mutation plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.
Claims20
A compound of Formula XIV:
- wherein:
- R1 and R2 are, independently, selected from the group consisting of H, OH, halogen, —C1-6alkyl, —C1-6fluoroalkyl, —CN, —NO2, —OR7, —SR7, —S(═O)R7, —S(═O)2R7, —NHS(═O)2R7, —C(═O)R7, —OC(═O)R7, —CO2R7, —OCO2R7, —CH(R7)2, —N(R7)2, —C(═O)N(R7)2, —NHC(═O)NHR7, —NHC(═O)R7, —NHC(═O)OR7, —C(OH)(R7)2, and —C(NH2)(R7)2;
- each R7 is, independently, H, halogen, or C1-C6alkyl, wherein the alkyl group is optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from halogen, OH, CN, and NO2;
- R3 is an optionally substituted aryl or an optionally substituted heteroaryl;
- R4, R5, and R6 are, independently, OH, —C1-10alkyl, —OC1-10alkyl, or —SC1-10alkyl, wherein each alkyl group is, independently, optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from halogen, OH, CN, and NO2;
- and
- n is an integer from 0 to 5;
- or an isomer, tautomer, or solvate thereof, or a pharmaceutically acceptable salt thereof;
- provided that:
- if n is 0, then R3 is not an optionally substituted pyrrolyl;
- and
- if n is 2, then the compound is not
9 more elements
(canceled)
Dependencies are inferred from the claim text.