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Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. III. Synthesis and Antitumor Activity of 3-Phenylpiperazinyl-1-trans-propenes

2005; Pharmaceutical Society of Japan; Volume: 53; Issue: 2 Linguagem: Inglês

10.1248/cpb.53.153

1347-5223

Hiroyuki Naito, Satoru Ohsuki, Ryo Atsumi, Megumi Minami, Mineko Mochizuki, Kenji Hirotani, Eiji Kumazawa, Akio Ejima,

Cancer therapeutics and mechanisms

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.