Development of 3-aryl-1-isoquinolinamines as potent antitumor agents based on CoMFA.
Various substituted 3-aryl-1-isoquinolinamines were designed and synthesized based on the previously constructed CoMFA model. Most of the synthesized compounds showed excellent potency in eight different human tumor cell lines as expected. In order to find the exact cytotoxic mechanism of these 3-aryl-1-isoquinolinamines, we analyzed the cell cycle dynamics by flow cytometry and found that 3-aryl-1-isoquinolinamine 6k-treated HeLa cells were arrested in G2/M phase, which is related to apoptosis.
Yang
Su Hui
SH
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Buk-gu, Gwangju 500-757, Korea.
Van
Hue Thi My
HT
Le
Thanh Nguyen
TN
Khadka
Daulat Bikram
DB
Cho
Suk Hee
SH
Lee
Kyung-Tae
KT
Lee
Eung-Seok
ES
Lee
Young Bok
YB
Ahn
Chang-Ho
CH
Cho
Won-Jea
WJ
D000588:Amines / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D005434:Flow Cytometry; D006801:Humans; D007546:Isoquinolines / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry
D000588:Amines; D000970:Antineoplastic Agents; D007546:Isoquinolines