Abstract
We synthesized 9alpha-fluoromedroxyprogesterone acetate (FMPA) in order to test whether it is a more potent anti-angiogenic agent than medroxyprogesterone acetate (MPA), which has been widely used as a therapeutic agent for breast and endometrium cancers. FMPA was previously synthesized in 10 steps (total yield: 1%). An efficient synthesis of FMPA has been achieved in 6 steps (total yield: 12%). We examined the anti-tumor effect of FMPA, complexed with dimethyl-beta-cyclodextrin (DM-beta-CyD), on rat mammary carcinomas induced by 7,12-dimethylbenz[a]anthracene (DMBA). FMPA showed great anti-tumor effect on DMBA-induced rat mammary carcinomas.
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / administration & dosage
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Carcinoma / drug therapy*
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Drug Screening Assays, Antitumor
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Female
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Fluorine / chemistry*
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Mammary Neoplasms, Experimental / drug therapy*
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Medroxyprogesterone Acetate / administration & dosage
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Medroxyprogesterone Acetate / analogs & derivatives*
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Medroxyprogesterone Acetate / chemical synthesis
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Medroxyprogesterone Acetate / chemistry
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Molecular Conformation
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Rats
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Rats, Sprague-Dawley
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Stereoisomerism
Substances
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9alpha-fluoromedroxyprogesterone acetate
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Antineoplastic Agents
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Fluorine
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Medroxyprogesterone Acetate