Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. III. Synthesis and Antitumor Activity of 3-Phenylpiperazinyl-1-trans-propenes
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概要
- 論文の詳細を見る
A series of novel 3-[4-phenyl-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes and related compounds were synthesized and evaluated by their cytotoxic activity against several tumor cell lines in vitro and in vivo antitumor activity against some tumor models when administered both intraperitoneally and orally. Compounds with the 3-chloropyridin-2-yl group (9g) and the 3-fluoro-5-substituted phenylpiperazinyl group (29b, c, and e) showed significantly potent cytotoxicity by in vitro testing. Among them, the 3-cyano-5-fluorophenyl derivative (29b) exhibited potent antitumor activity against several tumor cells including human carcinoma without causing undesirable effects in mice.
- 公益社団法人日本薬学会の論文
- 2005-02-01
著者
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KUMAZAWA Eiji
New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd.
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Atsumi R
Daiichi Pharmaceutical Co. Ltd. Tokyo Jpn
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Atsumi Ryo
Drug Metabolism & Physicochemical Property Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Atsumi Ryo
Drug Metabolism & Analytical Chemistry Research Center Developmental Research Laboratories Daiic
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Kumazawa E
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Naito H
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Naito Hiroyuki
Department Of Veterinary Science Azabu University
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Kumazawa Eiji
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Ejima A
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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NAITO Hiroyuki
Medicinal Chemistry Research Laboratory
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OHSUKI Satoru
Medicinal Chemistry Research Laboratory
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MINAMI Megumi
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.
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HIROTANI Kenji
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.
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EJIMA Akio
Medicinal Chemistry Research Laboratory
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Minami M
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Ohsuki S
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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Hirotani K
Discovery Research Laboratory Daiichi Pharmaceutical Co. Ltd.
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MOCHIZUKI Mineko
New Product Research Laboratories III, Daiichi Pharmaceutical Co. Ltd.
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HIROTANI Kenji
Discovery Research Laboratory, Daiichi Pharmaceutical Co. Ltd.
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Mochizuki Mineko
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Minami Megumi
New Product Research Laboratories III, Daiichi Pharmaceutical Co. Ltd.
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