• Title/Summary/Keyword: 3-Arylquinolin-2-ones

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Studies on the Synthesis and In Vitro Antitumor Activity of the Isoquinolone Derviatives

  • Cheon, Seung-Hoon;Lee, Joon-Yeol;Chung, Byung-Ho;Choi, Bo-Gil;Cho, Won-Jea;Kim, Tae-Sung
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.179-183
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    • 1999
  • 3-Arylisoquinolin-1(2H)-ones (2) are possible bioisosteres of the $5-[4^{l}-(piperidinomethyl)phenyl]-2<$,3-dihydroimidazo[2,1-$\alpha$]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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