KMID : 0043319990220020179
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Archives of Pharmacal Research 1999 Volume.22 No. 2 p.179 ~ p.183
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Studies on the Synthesis and In Vitro Antitumor Activity of the Isoquinolone Derviatives
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Cheon Seung-Hoon
Lee Joon-Yeol Chung Byung-Ho Choi Bo-Gil Cho Won-Jea Kim Tae-Sung
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Abstract
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3-Arylisoquinolin-1(2H)-ones (2) are possible bioisosteres of the $5-[4^{l}-(piperidinomethyl)phenyl]-2<$,3-dihydroimidazo[2,1-]isoquinoline (1) which is in clinical evaluation for the treatment of cancer. Structure-activity relationship studies of 3-arylisoquinolin-1(2H)-ones. (2) led to the synthesis of 3-arylquinolin-2(1H)-ones (3). A number of 3-phenyl substituted quinolin-2(1H)-ones were synthesized and tested for their in vitro antitumor activity against four different human tumor cell lines and 3-phenyl-N-benzyl-3,4-dihydroquinolin-2(1H)-one (12) showed the most potent activity.
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KEYWORD
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3-Arylisoquinolin-1-ones, 3-Arylquinolin-2-ones, Antitumor, Cytotoxicity
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