Synthesis and anti-tumor activity of a fluorinated analog of medroxyprogesterone acetate (MPA), 9alpha-fluoromedroxyprogesterone acetate (FMPA) |
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| Authors: | Murata Natsuko Fujimori Shiho Ichihara Yoshitatsu Sato Yoshio Yamaji Taketo Tsuboi Hiroshi Uchida Masayuki Suzuki Hiroto Yamada Masashi Oikawa Tsutomu Nemoto Hideo Nobuhiro Junko Choshi Tominari Hibino Satoshi |
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| Affiliation: | Pharmaceuticals Development Department, Meiji Dairies Corporation, Tokyo, Japan. natsuko_murata@meiji-milk.com |
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| 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. |
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