Abstract
Scaffold hybridization of several natural and synthetic anticancer leads led to the consideration of indenoindolones as potential novel anticancer agents. A series of these compounds were prepared by a diversity-feasible synthetic method. They were found to possess anticancer activities with higher potency compared to etoposide and 5-fluorouracil in kidney cancer cells (HEK 293) and low toxicity to corresponding normal cells (Vero). They exerted apoptotic effect with blocking of cell cycle at G2/M phase.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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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Apoptosis / drug effects*
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Biomarkers / metabolism
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Cell Survival / drug effects
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Chlorocebus aethiops
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Etoposide / pharmacology
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Flow Cytometry
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Fluorouracil / pharmacology
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G2 Phase Cell Cycle Checkpoints / drug effects*
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HEK293 Cells
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Humans
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Indenes / chemical synthesis*
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Indenes / pharmacology
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Inhibitory Concentration 50
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Vero Cells
Substances
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Antineoplastic Agents
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Biomarkers
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Indenes
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Indoles
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Etoposide
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Fluorouracil