Synthesis and structure-activity relationship studies of substituted isoquinoline analogs as antitumor agent.
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-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).
Cheon
S H
SH
College of Pharmacy, Chonnam National University, Kwangju, Korea.
Park
J S
JS
Chung
B H
BH
Choi
B G
BG
Cho
W J
WJ
Choi
S U
SU
Lee
C O
CO
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D007546:Isoquinolines