Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors.
Publication
, Journal Article
Xu, K; Xiao, Z; Tang, YB; Huang, L; Chen, C-H; Ohkoshi, E; Lee, K-H
Published in: Bioorg Med Chem Lett
April 15, 2012
Fourteen naphthoquinone derivatives (1-14) were designed based on a putative proteasome inhibitor PI-083. These compounds were synthesized and evaluated against A549, DU145, KB, and KBvin tumor cell lines. Six compounds (2, 4, 8, 9, 10, and 13) showed antiproliferative activities comparable to that of PI-083. Among them, compound 8 was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings endorse further optimization efforts based on this structural phenotype to develop potential anticancer drug candidates.
Duke Scholars
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Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
April 15, 2012
Volume
22
Issue
8
Start / End Page
2772 / 2774
Location
England
Related Subject Headings
- Proteasome Inhibitors
- Naphthoquinones
- Molecular Structure
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- Humans
- Drug Screening Assays, Antitumor
- Drug Design
- Cell Proliferation
Citation
APA
Chicago
ICMJE
MLA
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Xu, K., Xiao, Z., Tang, Y. B., Huang, L., Chen, C.-H., Ohkoshi, E., & Lee, K.-H. (2012). Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors. Bioorg Med Chem Lett, 22(8), 2772–2774. https://doi.org/10.1016/j.bmcl.2012.02.086
Xu, Kai, Zhiyan Xiao, Yan Bo Tang, Li Huang, Chin-Ho Chen, Emika Ohkoshi, and Kuo-Hsiung Lee. “Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors.” Bioorg Med Chem Lett 22, no. 8 (April 15, 2012): 2772–74. https://doi.org/10.1016/j.bmcl.2012.02.086.
Xu K, Xiao Z, Tang YB, Huang L, Chen C-H, Ohkoshi E, et al. Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2772–4.
Xu, Kai, et al. “Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors.” Bioorg Med Chem Lett, vol. 22, no. 8, Apr. 2012, pp. 2772–74. Pubmed, doi:10.1016/j.bmcl.2012.02.086.
Xu K, Xiao Z, Tang YB, Huang L, Chen C-H, Ohkoshi E, Lee K-H. Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2772–2774.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
April 15, 2012
Volume
22
Issue
8
Start / End Page
2772 / 2774
Location
England
Related Subject Headings
- Proteasome Inhibitors
- Naphthoquinones
- Molecular Structure
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- Humans
- Drug Screening Assays, Antitumor
- Drug Design
- Cell Proliferation