Abstract
We recently synthesized a series of novel makaluvamine compounds, and found that the most potent was FBA-TPQ. The effects of FBA-TPQ on human (LNCaP and PC3) and murine (TRAMP C1) prostate cancer cells were evaluated. Potential mechanisms of action of the compound were also determined. FBA-TPQ exhibited dose-dependent cytotoxicity in the low micromolar range, inhibited proliferation, caused cell cycle arrest, and induced apoptosis in prostate cancer cell lines. The compound also decreased the expression of the androgen receptor and PSA. The results presented herein support the further development of FBA-TPQ as a novel agent for prostate cancer.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / therapeutic use*
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Apoptosis / drug effects
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Cell Cycle / drug effects
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Gene Expression Regulation, Neoplastic / drug effects
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Humans
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Male
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Mice
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Prostate-Specific Antigen / metabolism
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Prostatic Neoplasms / drug therapy*
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Pyrroles / chemical synthesis
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Pyrroles / pharmacology
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Pyrroles / therapeutic use*
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Quinolones / chemical synthesis
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Quinolones / pharmacology
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Quinolones / therapeutic use*
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Receptors, Androgen / metabolism
Substances
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7-(4-fluorobenzylamino)-1,3,4,8-tetrahydropyrrolo(4,3,2-de)quinolin-8(1H)-one
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Antineoplastic Agents
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Pyrroles
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Quinolones
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Receptors, Androgen
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Prostate-Specific Antigen