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Original Article
Bo-Ya Shi
Yunnan Agricultural University
Corresponding Author
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This work is licensed under a CC BY 4.0 License. Read Full License
Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogues conjugated to the D-glucosyl azide were synthesized by carrying out the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, and were evaluated for their cytotoxicities against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Compounds 10 and 11 showed the highest levels of cytotoxicity against the HL-60 cells with IC50 values of 4.57 μM and 3.78 μM, respectively, and showed moderate selectivity towards cancer cell lines. Compound 11 was also shown to induce apoptosis in HL-60 cells. Most notably, inclusion of the perbutyrylated glucose residue in an EGCG derivative was concluded to lead to increased anticancer activity.
Keywords
EGCG, butyrylated glucosides, antitumor activity, CuAAC, synthesis
Figure 1
Figure 2
Figure 3
This is a list of supplementary files associated with this preprint. Click to download.
- Scheme1.jpg
Synthesis of the EGCG derivatives 10–13.
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CURRENT STATUS: Under Review
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Posted 11 Feb, 2021
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On 22 Feb, 2021
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Received 02 Feb, 2021
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This preprint is under consideration at Medicinal Chemistry Research. A preprint is a preliminary version of a manuscript that has not completed peer review at a journal. Research Square does not conduct peer review prior to posting preprints. The posting of a preprint on this server should not be interpreted as an endorsement of its validity or suitability for dissemination as established information or for guiding clinical practice.
Learn more about In Review
Original Article
Bo-Ya Shi
Yunnan Agricultural University
Corresponding Author
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
Peer Review Timeline
CURRENT STATUS: Under Review
Version 1
Posted 11 Feb, 2021
No community comments so far
Editorial decision: Major Revision
On 22 Feb, 2021
Reviews received
Received 02 Feb, 2021
Reviewers invited
Invitations sent on 02 Feb, 2021
Editor assigned
On 30 Jan, 2021
First submitted
On 25 Jan, 2021
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
Subject Areas
Medicinal Chemistry
License:
This work is licensed under a CC BY 4.0 License. Read Full License
Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogues conjugated to the D-glucosyl azide were synthesized by carrying out the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, and were evaluated for their cytotoxicities against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Compounds 10 and 11 showed the highest levels of cytotoxicity against the HL-60 cells with IC50 values of 4.57 μM and 3.78 μM, respectively, and showed moderate selectivity towards cancer cell lines. Compound 11 was also shown to induce apoptosis in HL-60 cells. Most notably, inclusion of the perbutyrylated glucose residue in an EGCG derivative was concluded to lead to increased anticancer activity.
Figure 1
Figure 2
Figure 3
This is a list of supplementary files associated with this preprint. Click to download.
- Scheme1.jpg
Synthesis of the EGCG derivatives 10–13.
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