Archives of Pharmacal Research

  • 제22권2호
  • /
  • Pages.179-183
  • /
  • 1999
  • /
  • 0253-6269(pISSN)
  • /
  • 1976-3786(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

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

  • Cheon, Seung-Hoon (College of Pharmacy, Chonnam National University, and Research Institute of Drug Development, Chonnam National University) ;
  • Lee, Joon-Yeol (College of Pharmacy, Chonnam National University, and Research Institute of Drug Development, Chonnam National University) ;
  • Chung, Byung-Ho (College of Pharmacy, Chonnam National University, and Research Institute of Drug Development, Chonnam National University) ;
  • Choi, Bo-Gil (College of Pharmacy, Chonnam National University, and Research Institute of Drug Development, Chonnam National University) ;
  • Cho, Won-Jea (College of Pharmacy, Chonnam National University, and Research Institute of Drug Development, Chonnam National University) ;
  • Kim, Tae-Sung (College of Pharmacy, Chonnam National University, and Research Institute of Drug Development, Chonnam National University)
  • 발행 : 1999.04.01
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초록

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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