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Title: Synthesis and structure-activity relationship of mono-indole-, bis-indole-, and tris-indole-based sulfonamides as potential anticancer agents
Authors: Pingaew R.
Prachayasittikul S.
Ruchirawat S.
Prachayasittikul V.
Keywords: antineoplastic agent
sulfonyl bis indole derivative
sulfonyl mono indole derivative
sulfonyl tris indole derivative
unclassified drug
antineoplastic activity
antiproliferative activity
controlled study
drug screening
drug synthesis
human cell
IC 50
priority journal
structure activity relation
Antineoplastic Agents
Carcinoma, Hepatocellular
Cell Line, Tumor
Cell Proliferation
Drug Screening Assays, Antitumor
Hep G2 Cells
Liver Neoplasms
Lung Neoplasms
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Structure-Activity Relationship
Issue Date: 2013
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.
ISSN: 13811991
Appears in Collections:SCOPUS 1983-2021

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