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Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. III. Synthesis and antitumor activity of 3-phenylpiperazinyl-1-trans-propenes. | LitMetric

AI Article Synopsis

  • - A series of novel compounds were developed that feature specific chemical structures, designed for potential cancer treatment, and were tested for their effectiveness against cancer cell lines.
  • - Specific compounds containing the 3-chloropyridin-2-yl and 3-fluoro-5-substituted phenylpiperazinyl groups demonstrated strong cytotoxic activity in lab tests.
  • - Among these, the 3-cyano-5-fluorophenyl derivative (29b) showed impressive antitumor effects on various cancer cells, including human carcinoma, while being safe for use in mice.

Article 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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Source
http://dx.doi.org/10.1248/cpb.53.153DOI Listing

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