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KMID : 0043319970200020138
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Archives of Pharmacal Research
1997 Volume.20 No. 2 p.138 ~ p.143
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Synthesis and Structure-Activity Relationship Studies of 2,3-Dihydroimidazo[2,1-a]isoquinoline Analogs as Antitumor Agents
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Cheon Seung-Hoon
Park Joon-Suck
Jeong Seon-Hee
Chung Byung-Ho
Choi Bo-Gil
Cho Won-Jea
Kang Boo-Hyon
Lee Chong-Ock
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Abstract
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5-Aryl-2,3-dihydroimidazo[2,1-a]isoquinolines were reported to have strong antitumor activity and one of the derivatives such as -(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, -(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.
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KEYWORD
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imidazoisoquinolines, Antitumor, SDZ 62-434
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