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Synthesis and Structure-Activity Relationship Studies of 2,3-Dihydroimidazo[2,1-a]isoquinoline Analogs as Antitumor Agents

Cheon, Seung-Hoon   (College of Pharmacy, Chonnam National UniversityUU0001112  ); Park, Joon-Suck   (College of Pharmacy, Chonnam National UniversityUU0001112  ); Jeong, Seon-Hee   (College of Pharmacy, Chonnam National UniversityUU0001112  ); Chung, Byung-Ho   (College of Pharmacy, Chonnam National UniversityUU0001112  ); Choi, Bo-Gil   (College of Pharmacy, Chonnam National UniversityUU0001112  ); Cho, Won-Jae   (College of Pharmacy, Chonnam National UniversityUU0001112  ); Kang, Boo-Hyon   (Screening and Toxicology Research Center, Korea Research Institute of Chemical TechnologyCC0186998  ); Lee, Chong-Ock   (Screening and Toxicology Research Center, Korea Research Institute of Chemical TechnologyCC0186998  );
  • 초록

    5-Aryl-2,3-dihydroimidazo[2,1-a]isoquinolines were reported to have strong antitumor activity and one of the derivatives such as $5-[4^{l}$ -(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1-a] isoquinoline (1, SDZ 62-434) was found to be more effective than the clinical cytostatic agent edelfosine (2) in in vitro and in vivo assays. Currently SDZ 62-434 is in clinical trials in Europe. The structure-activity relationship studies of SDZ 62-434 showed that compounds with substitution on ring A were less active than the lead compound. Ring B in SDZ 62-434 was essential for the activity because compounds without B ring had no antitumor activity. Among the 3-arylisoquinolin-1-one derivatives, $3-[4^{I}$ -(piperidinomethyl)phenyl] substituted analog had no antitumor activity but simple phenyl substituted compound, such as 4, showed the most potent antitumor activity in various human tumor cell lines.


  • 주제어

    imidazoisoquinolines .   Antitumor .   SDZ 62-434.  

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  • Park, Joon-Suck (1)

  • 정병호 (23)

  • Choi, Bo-Gil (24)

  • Cho, Won-Jea (19)

  • 강부현 (29)

  • 이정옥 (45)

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