Emetine Derivatives, Prodrugs Containing Same, And Methods Of Treating Conditions Using Same
OwnerOladapo Bakareinventor
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Abstract
Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.
Claims11
A compound comprising formula (I):
- where M is selected from the group consisting of:
- and where:
- X1═H, —NO2, —CO2X2, −OX3, halogen, or C1-C4 alkyl,
- X2 ═C1-C4 alkyl or H,
- X3═C1-C4 alkyl or H,
- Q=OH, V+O—,
- V=metal ion,
- Y═H or C1-C6 alkyl,
- Z═H, C1-C4 alkyl, or halogen,
- p=0 to 8, and
- t=1 to 4.
A compound comprising formula (I)
- where M has the general formula:
- and where V is a metal ion.
A compound comprising formula (I):
- where M has the general formula:
- where R8 is selected from the group consisting of:
- where
- L=H2N— and H3CO—
- m=1-3.
- n=0-1,
- p=0 to 8,
- X1═H, —NO2, —CO2X2, —OX3, halogen, or C1-C4 alkyl,
- X2═C1-C4 alkyl or H, and
- X3═C1-C4 alkyl or H.
A compound comprising formula (I):
- where M is not hydrogen and comprises a substituent effective to be hydrolyzed by an enzyme preferentially expressed by cancer cells.
(canceled)
11-15. (canceled)
Dependencies are inferred from the claim text.