Chemical and Pharmaceutical Bulletin p. 1679 - 1684 (1999)
Update date:2022-08-02
Topics:
Naito, Hiroyuki
Sugimori, Masamichi
Mitsui, Ikuo
Nakamura, Yoshihide
Iwahana, Michio
Ishii, Mineko
Hirotani, Kenji
Kumazawa, Eiji
Ejima, Akio
Novel pyrimidinyl pyrazole derivatives were synthesized and examined for cytotoxic and antitumor activity. Mannich reaction was employed to construct this scaffold. Among the compounds synthesized, a series of propene derivatives exhibited a potent cytotoxic activity against some tumor cell lines including multidrug resistant cell lines due to the overexpression of P-glycoprotein. The vinyl bond moiety in the scaffold was believed to be required for the cytotoxic activity. Among them, compound 14g, when administered intraperitoneaily, showed potent antitumor activity against the malignant ascites caused by intraperitoneal inoculation of P388 cells in mice. This compound also showed high activity against a solid tumor Meth A mouse fibrosarcoma when administered both intraperitoneaily and orally.
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Doi:10.1016/S0957-4166(99)00493-0
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(2005)Doi:10.1016/S0968-0896(99)00223-0
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(2014)
