178928-29-5Relevant academic research and scientific papers
Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. II. Optimization of the phenylpiperazine moiety of 1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes.
Naito, Hiroyuki,Ohsuki, Satoru,Sugimori, Masamichi,Atsumi, Ryo,Minami, Megumi,Nakamura, Yoshihide,Ishii, Mineko,Hirotani, Kenji,Kumazawa, Eiji,Ejima, Akio
, p. 453 - 462 (2007/10/03)
A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propene (2) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines in vitro and antitumor activity against some tumor models when dosed both intraperitoneally and orally in vivo. Compounds 7a and 7e, the 3,5-difluorophenyl and 3,5-dichlorophenyl analogues of 2, respectively, showed significantly more potent cytotoxicity than 2 in vitro and potent antitumor activities without causing decrease of body temperature related to side effects.
Pyrimidinylpyrazole derivatives
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, (2008/06/13)
The present invention provides a novel compound which is represented by formula (I): STR1 wherein preferable examples of R1 to R6 are as follows; R1 and R2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R3 is a hydrogen atom; R4 is a methyl group; R5 is a hydrogen atom or an alkyl group; and R6 is a group of the formula: STR2 wherein Z is a phenyl group; and has an antitumor effect.
