Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. III. Synthesis and antitumor activity of 3-phenylpiperazinyl-1-trans-propenes.
Chem Pharm Bull (Tokyo)
; 53(2): 153-63, 2005 Feb.
Article
in En
| MEDLINE
| ID: mdl-15684512
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Piperazines
/
Propane
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Chem Pharm Bull (Tokyo)
Year:
2005
Document type:
Article
Affiliation country:
Japan
Country of publication:
JAPAN
/
JAPON
/
JAPÃO
/
JP