Abstract
A series of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs, 3f and 3j had IC(50) values of 4.4 and 5.2microM, respectively, compared to 5-fluorouracil (IC(50)=15.2microM) against MCF-7 cells.
Copyright 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects*
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Cell Survival / drug effects*
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Drug Design
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Drug Screening Assays, Antitumor / methods*
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Humans
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Imidazolidines / chemical synthesis
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Imidazolidines / pharmacology*
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Indoles / chemistry
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Inhibitory Concentration 50
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Structure-Activity Relationship
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Tryptophan / analogs & derivatives*
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Tryptophan / chemical synthesis
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Tryptophan / chemistry
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Tryptophan / pharmacology
Substances
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Antineoplastic Agents
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Imidazolidines
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Indoles
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imidazolidine-2,4-dione
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aplysinopsin
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Tryptophan