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

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...

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Published inMarine drugs Vol. 9; no. 2; p. 256
Main Authors Shen, Ya-Ching, Chang, Yao-To, Lin, Chun-Ling, Liaw, Chia-Ching, Kuo, Yao Haur, Tu, Lan-Chun, Yeh, Sheau Farn, Chern, Ji-Wang
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 01.02.2011
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Summary: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 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.
ISSN:1660-3397
DOI:10.3390/md9020256