Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. III. Synthesis and Antitumor Activity of 3-Phenylpiperazinyl-1-trans-propenes
| Autor: | Eiji Kumazawa, Megumi Minami, Hiroyuki Naito, Ryo Atsumi, Satoru Ohsuki, Akio Ejima, Mineko Mochizuki, Kenji Hirotani |
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| Rok vydání: | 2005 |
| Předmět: |
Magnetic Resonance Spectroscopy
Chemical Phenomena Stereochemistry Mice Nude Antineoplastic Agents Pyrazole Pharmacology Piperazines Mice Propane Structure-Activity Relationship chemistry.chemical_compound In vivo Cell Line Tumor Drug Discovery Animals Humans Cytotoxic T cell Structure–activity relationship Cytotoxicity Antitumor activity Mice Inbred BALB C Chemistry Physical General Chemistry General Medicine Nuclear magnetic resonance spectroscopy In vitro chemistry Drug Screening Assays Antitumor Neoplasm Transplantation |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 53:153-163 |
| ISSN: | 1347-5223 0009-2363 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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