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Mar. Drugs 2011, 9(2), 256-277; doi:10.3390/md9020256

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

1
School of Pharmacy, National Taiwan University, Taipei 100, Taiwan
2
National Research Institute of Chinese Medicine, Taipei 112, Taiwan
3
Institute of Biochemistry, National Yang-Ming University, Taipei 112, Taiwan
*
Author to whom correspondence should be addressed.
Received: 30 December 2010 / Revised: 31 January 2011 / Accepted: 7 February 2011 / Published: 10 February 2011
(This article belongs to the Special Issue Marine Alkaloids)
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Abstract

A series of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-b-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 114 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.
Keywords: carbazolyl-1,2,3,4-tetrahydro-b-carbolines; carbazolyl-3,4-dihydro-b-carbolines; antitumor agents; structure activity relationship carbazolyl-1,2,3,4-tetrahydro-b-carbolines; carbazolyl-3,4-dihydro-b-carbolines; antitumor agents; structure activity relationship
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Shen, Y.-C.; Chang, Y.-T.; Lin, C.-L.; Liaw, C.-C.; Kuo, Y.H.; Tu, L.-C.; Yeh, S.F.; Chern, J.-W. Synthesis of 1-Substituted Carbazolyl-1,2,3,4-tetrahydro- and Carbazolyl-3,4-dihydro-β-carboline Analogs as Potential Antitumor Agents. Mar. Drugs 2011, 9, 256-277.

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