Studies on the synthesis andin vitro antitumor activity of the isoquinolone derivatives |
| |
Authors: | Seung Hoon Cheon Joon Yeol Lee Byung-Ho Chung Bo-Gil Choi Won-Jea Cho Tae Sung Kim |
| |
Affiliation: | College of Pharmacy, Chonnam National University, Kwangju, Korea. shcheon@chonnam.chonnam.ac.kr |
| |
Abstract: | 3-Arylisoquinolin-1(2H)-ones (2) are possible bioisosteres of the 5-[4'-(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1-a]iso quinoline (1) which is in clinical evaluation for the treatment of cancer. Structure-activity relationship studies of 3-arylisoquinolin-1(2H)-ones (2) led to the synthesis of 3-arylquinolin-2(1H)-ones (3). A number of 3-phenyl substituted quinolin-2(1H)-ones were synthesized and tested for their in vitro antitumor activity against four different human tumor cell lines and 3-phenyl-N-benzyl-3,4-dihydroquinolin-2(1H)-one (12) showed the most potent activity. |
| |
Keywords: | 3-Arylisoquinolin-1-ones 3-Arylquinolin-2-ones Antitumor Cytotoxicity |
本文献已被 PubMed SpringerLink 等数据库收录! |