Abstract
A new family of microtubule-targeting agents with a phenothiazine A-ring was synthesized and evaluated for anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferation and tubulin polymerization, rather similar to those of phenstatin. Phenothiazine derivative 21 proved to be the most potent compound synthesized with GI(50) values ranging from 29 to 93 nM on different cell lines. The same compound showed a better inhibition of COLO 205, A498, and MCF7 cell lines than the parent phenstatin.
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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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / toxicity
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Binding Sites
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor
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Humans
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MCF-7 Cells
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Molecular Docking Simulation
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Phenothiazines / chemical synthesis*
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Phenothiazines / chemistry
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Phenothiazines / toxicity
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Polymerization / drug effects
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Protein Structure, Tertiary
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Structure-Activity Relationship
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Tubulin / chemistry*
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Tubulin / metabolism
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Tubulin Modulators / chemical synthesis*
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Tubulin Modulators / chemistry
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Tubulin Modulators / toxicity
Substances
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Antineoplastic Agents
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Phenothiazines
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Tubulin
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Tubulin Modulators