Synthesis and Structure-Activity Relationship Studies of Substituted Isoquinoline Analogs Antitumor Agent

  • Cheon, Seung-Hoon (College of Pharmacy, Chonnam National Uuniversity) ;
  • Park, Joon-Suck (College of Pharmacy, Chonnam National Uuniversity) ;
  • Chung, Byung-Ho (College of Pharmacy, Chonnam National Uuniversity) ;
  • Choi, Bo-Gil (College of Pharmacy, Chonnam National Uuniversity) ;
  • Cho, Won-Jae (College of Pharmacy, Chonnam National Uuniversity) ;
  • Choi, Sang-Un (Screening and Toxicology Research Center, Korea Research Institute of Chemical Technology) ;
  • Lee, Chong-Ock (Screening and Toxicology Research Center, Korea Research Institute of Chemical Technology)
  • Published : 1998.04.01

Abstract

A number of substituted isoquinolin-1-ones, possible bioisosteres of the 5-aryl substituted 2,3-dihydroimidazo[2,$1-a$]isoquinolines, were synthesized and tested for their antitumor activity against five different human tumor cell lines. O-(3-hydroxyporpyl) substituted compound (15) exhibited the best antitumor activity which is 3-5 times better than 5-[$4^1$-(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,$1-a$]isoquinoline (1).

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