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DC Field | Value | Language |
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dc.contributor.author | Pingaew R. | |
dc.contributor.author | Prachayasittikul S. | |
dc.contributor.author | Ruchirawat S. | |
dc.contributor.author | Prachayasittikul V. | |
dc.date.accessioned | 2021-04-05T03:32:52Z | - |
dc.date.available | 2021-04-05T03:32:52Z | - |
dc.date.issued | 2013 | |
dc.identifier.issn | 13811991 | |
dc.identifier.other | 2-s2.0-84880829458 | |
dc.identifier.uri | https://ir.swu.ac.th/jspui/handle/123456789/14024 | - |
dc.identifier.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84880829458&doi=10.1007%2fs11030-013-9457-7&partnerID=40&md5=f954dc5a8a04272b455f3e4346568f8a | |
dc.description.abstract | A series of arylsulfonyl mono-indoles (10-15), bis-indoles (16-27), and tris-indoles (28-32) have been synthesized and evaluated for their cytotoxicity toward four human cancer cell lines including HuCCA-1 (cholangiocarcinoma), HepG2 (hepatocellular carcinoma), A-549 (lung carcinoma), and MOLT-3 (lymphoblastic leukemia). Most of the synthesized indoles displayed cytotoxicity against the MOLT-3 cell line except for analogs 16, 17, and 32. Significantly, the NN -sulfonylphenolic bis-indole series (18-27) and the NN -chlorobenzenesulfonyl tris-indole (30) showed higher antiproliferative activity against HepG2 cell than the reference drug, etoposide. Promisingly, the NN -chlorobenzenesulfonyl bis-indole (20) and tris-indole (30) provided 3-fold and 2-fold stronger activity, respectively, against HepG2 cell than etoposide. Moreover, the phenolic bis-indole (20) was also shown to be the most potent cytotoxic agent against HuCCA-1 and A-549 cell lines with IC50 values of 7.75 and 8.74 μ M, respectively. The tris-indole analogs 28, 29, and 31 also exhibited selectivity against MOLT-3 cell. The findings disclosed that NN -arylsulfonyl bis-indoles-bearing phenolic groups are potentially interesting lead pharmacophores of anticancer agents that should be further investigated in more detail. © 2013 Springer Science+Business Media Dordrecht. | |
dc.subject | antineoplastic agent | |
dc.subject | sulfonamide | |
dc.subject | sulfonyl bis indole derivative | |
dc.subject | sulfonyl mono indole derivative | |
dc.subject | sulfonyl tris indole derivative | |
dc.subject | unclassified drug | |
dc.subject | antineoplastic activity | |
dc.subject | antiproliferative activity | |
dc.subject | article | |
dc.subject | controlled study | |
dc.subject | drug screening | |
dc.subject | drug synthesis | |
dc.subject | human | |
dc.subject | human cell | |
dc.subject | IC 50 | |
dc.subject | priority journal | |
dc.subject | structure activity relation | |
dc.subject | Antineoplastic Agents | |
dc.subject | Arylsulfonates | |
dc.subject | Carcinoma, Hepatocellular | |
dc.subject | Cell Line, Tumor | |
dc.subject | Cell Proliferation | |
dc.subject | Cholangiocarcinoma | |
dc.subject | Drug Screening Assays, Antitumor | |
dc.subject | Hep G2 Cells | |
dc.subject | Humans | |
dc.subject | Indoles | |
dc.subject | Liver Neoplasms | |
dc.subject | Lung Neoplasms | |
dc.subject | Neoplasms | |
dc.subject | Precursor Cell Lymphoblastic Leukemia-Lymphoma | |
dc.subject | Structure-Activity Relationship | |
dc.subject | Sulfonamides | |
dc.title | Synthesis and structure-activity relationship of mono-indole-, bis-indole-, and tris-indole-based sulfonamides as potential anticancer agents | |
dc.type | Article | |
dc.rights.holder | Scopus | |
dc.identifier.bibliograpycitation | Molecular Diversity. Vol 17, No.3 (2013), p.595-604 | |
dc.identifier.doi | 10.1007/s11030-013-9457-7 | |
Appears in Collections: | Scopus 1983-2021 |
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