HYDROXY-SUBSTITUTED GOLD(III) PORPHYRIN COMPLEXES AS HISTONE DEACETYLASE INHIBITORS
A method for treatment of cancer by inhibiting the activity of histone deacetylase, comprising administering to a human in need of such treatment a composition containing a therapeutically effective amount of a gold(III) complex having the structural formula of ##STR00001## or a pharmaceutically acceptable salt thereof, wherein: --R is selected from the group consisting of --OH, --CH.sub.2OH, C.sub.2H.sub.4OH, --C.sub.3H.sub.6OH or --C.sub.4H.sub.8OH; and X is independently a pharmaceutically acceptable counter-ion.
Inventor: CHE, Chiming | WANG, Yu | SUN, Waiyin, Raymond | CHOW, Heiman, Kim
Priority Number: EP2493897B1
IPC Current: C07F000112 | A61K003128 | A61P003500 | C07D048722
Assignee Applicant: The University of Hong Kong
Title: HYDROXY-SUBSTITUTED GOLD(III) PORPHYRIN COMPLEXES AS HISTONE DEACETYLASE INHIBITORS | HYDROXY-SUBSTITUIERTE GOLD-(III-)PORPHYRIN-KOMPLEXE ALS HISTONDEACETYLASEHEMMER | COMPLEXES HYDROXY-SUBSTITUÉS DE PORPHYRINE D'OR (III) UTILISABLES EN TANT QU'INHIBITEUR
Usefulness: HYDROXY-SUBSTITUTED GOLD(III) PORPHYRIN COMPLEXES AS HISTONE DEACETYLASE INHIBITORS | HYDROXY-SUBSTITUIERTE GOLD-(III-)PORPHYRIN-KOMPLEXE ALS HISTONDEACETYLASEHEMMER | COMPLEXES HYDROXY-SUBSTITUÉS DE PORPHYRINE D'OR (III) UTILISABLES EN TANT QU'INHIBITEURS DE L'HISTONE DÉSACÉTYLASE
Summary: (I) is useful for treating cancer, where: (I) induces apoptosis in cancer cells; and the cancer includes cervical epithelioid carcinoma, hepatocellular carcinoma, leukemia, nasopharyngeal carcinoma, breast carcinoma, melanoma and/or lung carcinoma (all claimed). The cytostatic effect of (I) was tested in five types of human breast carcinoma cells with distinct gene expression profiles and oncogenic phenotypes, including BT474, MCF-7, T47D, MDA-MB-231 and SKBR3. The results showed that the IC 50 value of gold(III) porphyrin complex of formula (Ia) was 0.49± 0.17 μ m, 0.08± 0.04 μ m, 0.04± 0.01 μ m, 0.007± 0.002 μ m and 0.02± 0.01 μ m, respectively.
Novelty: Treating cancer (e.g. cervical epithelioid carcinoma, hepatocellular carcinoma, breast carcinoma and/or lung carcinoma) comprises administering composition comprising new or known substituted gold(III) porphyrin complexes
診斷/治療
癌症/腫瘤
12/913,398
美國
