Synthesis of 1-Substituted Carbazolyl-1,2,3,4-tetrahydro- and Carbazolyl-3,4-dihydro-β-carboline Analogs as Potential Antitumor Agents

Marine Drugs

Ya-Ching Shen¹  Yao-To Chang¹  Chun-Ling Lin¹  Chia-Ching Liaw¹  Yao Haur Kuo³  Lan-Chun Tu²  Sheau Farn Yeh² 

[1] School of Pharmacy, National Taiwan University, Taipei 100, Taiwan; E-Mails:;Institute of Biochemistry, National Yang-Ming University, Taipei 112, Taiwan; E-Mail:;National Research Institute of Chinese Medicine, Taipei 112, Taiwan; E-Mail:

关键词: carbazolyl-1;    2;    3;    4-tetrahydro-β-carbolines;    carbazolyl-3;    4-dihydro-β-carbolines;    antitumor agents;    structure activity relationship;   

DOI  :  10.3390/md9020256

来源: mdpi

【 摘 要 】

A series of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-β-carboline analogs have been synthesized and evaluated for antitumor activity against human tumor cells including KB, DLD, NCI-H661, Hepa, and HepG2/A2 cell lines. Among these, compounds 2, 6, 7, and 9 exhibited the most potent and selective activity against the tested tumor cells. As for inhibition of topoisomerase II, compounds 1–14 and 18 showed better activity than etoposide. Among them, compounds 3, 4, 7, 9, and 10 exhibited potent activity. The structure and activity relationship (SAR) study revealed correlation between carbon numbers of the side chain and biological activities. The molecular complex with DNA for compound 2 was proposed.

【 授权许可】

CC BY   
© 2011 by the authors; licensee MDPI, Basel, Switzerland.