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Synthesis and structure-activity relationship studies of substituted isoquinoline analogs as antitumor agent

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

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Correspondence to Seung Hoon Cheon.

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Cheon, S.H., Park, J.S., Chung, B. et al. Synthesis and structure-activity relationship studies of substituted isoquinoline analogs as antitumor agent. Arch. Pharm. Res. 21, 193–197 (1998).

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Key words

  • Isoquinolin-1-ones
  • Antitumor
  • Bioisostere