Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. II. Optimization of the Phenylpiperazine Moiety of 1- [5-Methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes
スポンサーリンク
概要
- 論文の詳細を見る
A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propene (2) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines in vitro and antitumor activity against some tumor models when dosed both intraperitoneally and orally in vivo. Compounds 7a and 7e, the 3,5-difluorophenyl and 3,5-dichlorophenyl ana-logues of 2, respectively, showed significantly more potent cytotoxicity than 2 in vitro and potent antitumor activities without causing decrease of body temperature related to side effects.
- 公益社団法人日本薬学会の論文
- 2002-04-01
著者
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中村 康彦
Department Of Formulation Research Dainippon Pharmaceutical Co. Ltd.
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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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Nakamura Yoshihide
Technical Department Fuji Chemical Industries Co. Ltd.
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Nakamura Y
Tohoku Pharmaceutical Univ. Sendai Jpn
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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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SUGIMORI Masamichi
Discovery Research Laboratory
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MINAMI Megumi
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.
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ISHII Mineko
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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Ishii M
Department Of Physical Chemistry Graduate School Of Pharmaceutical Sciences Chiba University
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Mitsui Ikuo
New Product Research Laboratories Iv Daiichi Pharmaceitucal Co. Ltd.
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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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Nakamura Y
Department Of Pharmacognosy Tohoku Pharmaceutical University
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Minami Megumi
New Product Research Laboratories III, Daiichi Pharmaceutical Co. Ltd.
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