synthesis of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-β-carboline analogs as potential antitumor agents合成1-substituted carbazolyl-1,2、3、4-tetrahydro carbazolyl-3,4-dihydro-β-carboline类似物作为潜在的抗肿瘤药物.pdfVIP

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synthesis of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-β-carboline analogs as potential antitumor agents合成1-substituted carbazolyl-1,2、3、4-tetrahydro carbazolyl-3,4-dihydro-β-carboline类似物作为潜在的抗肿瘤药物.pdf

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synthesis of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-β-carboline analogs as potential antitumor agents合成1-substituted carbazolyl-1,2、3、4-tetrahydro carbazolyl-3,4-dihydro-β-carboline类似物作为潜在的抗肿瘤药物

Mar. Drugs 2011, 9, 256-277; doi:10.3390/md9020256 OPEN ACCESS Marine Drugs ISSN 1660-3397 /journal/marinedrugs Article Synthesis of 1-Substituted Carbazolyl-1,2,3,4-tetrahydro- and Carbazolyl-3,4-dihydro-β-carboline Analogs as Potential Antitumor Agents Ya-Ching Shen 1,*, Yao-To Chang 1, Chun-Ling Lin 1, Chia-Ching Liaw 1, Yao Haur Kuo 2, 3 3 1 Lan-Chun Tu , Sheau Farn Yeh and Ji-Wang Chern 1 School of Pharmacy, National Taiwan University, Taipei 100, Taiwan; E-Mails: ato@ (Y.-T.C.); 6850101@ (C.-L.L.); biogodas@ (C.-C.L.); jwchern @.tw (J.-W.C.) 2 National Research Institute of Chinese Medicine, Taipei 112, Taiwan; E-Mail: kuoyh@.tw 3 Institute of Biochemistry, National Yang-Ming University, Taipei 112, Taiwan; E-Mail: fyeh@.tw (S.F.Y.) * Author to whom correspondence should be addressed; E-Mail: ycshen@.tw; Tel.: +886-2(ext.) 62226; Fax: +886-2 Received: 30 December 2010; in revised form: 31 January 2011 / Accepted: 7 February 2011 / Published: 10 February 2011 Abstract: A series of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4- dihydro--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,