Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. III. Synthesis and Antitumor Activity of 3-Phenylpiperazinyl-1-trans-propenes
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- Naito Hiroyuki
- Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co. Ltd.
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- Ohsuki Satoru
- Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co. Ltd.
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- Atsumi Ryo
- Drug Metabolism & Physicochemical Property Research Laboratory, Daiichi Pharmaceutical Co. Ltd.
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- Minami Megumi
- New Product Research Laboratories III, 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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- Kumazawa Eiji
- New Product Research Laboratories III, Daiichi Pharmaceutical Co. Ltd.
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- Ejima Akio
- Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co. Ltd.
Bibliographic Information
- Other Title
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- Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives(3)Synthesis and Antitumor Activity of 3-Phenylpiperazinyl-1-trans-propenes
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Abstract
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.
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 53 (2), 153-163, 2005
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390001204169072768
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- NII Article ID
- 130000109754
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 7233534
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- PubMed
- 15684512
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed