Discovery of a potent and highly fluorescent sirtuin inhibitorElectronic supplementary information (ESI) available: Compound characterization data, supplementary biological data, additional photochemical measurements and molecular docking analyses. See DOI: 10.1039/c5md00307e
In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series ( BZD9L1 ) was discovered to show high autofluorescence which can be utilized to predict its localization in cell...
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| Main Authors | , , , , , |
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| Format | Journal Article |
| Language | English |
| Published |
08.10.2015
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| Online Access | Get full text |
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| Abstract | In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (
BZD9L1
) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly,
BZD9L1
displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.
Highly fluorescent sirtuin inhibitor was discovered to possess growth inhibitory effect against multiple cancer cell lines. |
|---|---|
| AbstractList | In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (
BZD9L1
) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly,
BZD9L1
displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.
Highly fluorescent sirtuin inhibitor was discovered to possess growth inhibitory effect against multiple cancer cell lines. |
| Author | Parang, K Choon, T. S Wei, A. C Shirazi, A. N Yoon, Y. K Ali, M. A |
| AuthorAffiliation | Institute for Research in Molecular Medicine University of Rhode Island Department of Biomedical and Pharmaceutical Sciences College of Pharmacy Universiti Sains Malaysia |
| AuthorAffiliation_xml | – name: Universiti Sains Malaysia – name: University of Rhode Island – name: Department of Biomedical and Pharmaceutical Sciences – name: College of Pharmacy – name: Institute for Research in Molecular Medicine |
| Author_xml | – sequence: 1 givenname: Y. K surname: Yoon fullname: Yoon, Y. K – sequence: 2 givenname: M. A surname: Ali fullname: Ali, M. A – sequence: 3 givenname: A. C surname: Wei fullname: Wei, A. C – sequence: 4 givenname: T. S surname: Choon fullname: Choon, T. S – sequence: 5 givenname: A. N surname: Shirazi fullname: Shirazi, A. N – sequence: 6 givenname: K surname: Parang fullname: Parang, K |
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| DOI | 10.1039/c5md00307e |
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| Notes | 10.1039/c5md00307e Electronic supplementary information (ESI) available: Compound characterization data, supplementary biological data, additional photochemical measurements and molecular docking analyses. See DOI |
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| Snippet | In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most... |
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| Title | Discovery of a potent and highly fluorescent sirtuin inhibitorElectronic supplementary information (ESI) available: Compound characterization data, supplementary biological data, additional photochemical measurements and molecular docking analyses. See DOI: 10.1039/c5md00307e |
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