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Page 1
Identification of Novel 4'-O-Demethyl-epipodophyllotoxin Derivatives as Antitumor Agents Targeting Topoisomerase II.
Xi W, Sun H, Bastow KF, Xiao Z, Lee KH. Xi W, et al. Molecules. 2022 Aug 7;27(15):5029. doi: 10.3390/molecules27155029. Molecules. 2022. PMID: 35956979 Free PMC article.
Four of the compounds (11, 18, 27 and 28) induced protein-linked DNA break (PLDB) levels higher than those of GL-331 (6) and 2, and are assumed to be topoisomerase II (topo II) poisons more potent than 6 and 2. ...
Four of the compounds (11, 18, 27 and 28) induced protein-linked DNA break (PLDB) levels higher than those of GL-331 (6) and 2 …
DNA damage and apoptosis induced by a potent orally podophyllotoxin derivative in breast cancer.
Wang Y, Sun H, Xiao Z, Zhang G, Zhang D, Bao X, Li F, Wu S, Gao Y, Wei N. Wang Y, et al. Cell Commun Signal. 2018 Sep 3;16(1):52. doi: 10.1186/s12964-018-0263-9. Cell Commun Signal. 2018. PMID: 30176902 Free PMC article.
RESULTS: The cytotoxicity of XWL-1-48 is more potent than that of its congener GL331. Molecular docking demonstrated that XWL-1-48 could bind to TopoII through forming two strong hydrogen bonds and potential pi-pi interactions. ...
RESULTS: The cytotoxicity of XWL-1-48 is more potent than that of its congener GL331. Molecular docking demonstrated that XWL-1-48 co …
XWL-1-48 exerts antitumor activity via targeting topoisomerase II and enhancing degradation of Mdm2 in human hepatocellular carcinoma.
Wang Y, Sun H, Xiao Z, Zhang D, Bao X, Wei N. Wang Y, et al. Sci Rep. 2017 Aug 30;7(1):9989. doi: 10.1038/s41598-017-10577-7. Sci Rep. 2017. PMID: 28855652 Free PMC article.
Moreover, the cytotoxicity of XWL-1-48 is more potent than its congener GL331 and the IC(50) values are from 0.34 0.21 to 3.54 0.54 M in 10 cancer cell lines including KBV200 cells with P-gp overexpression. ...
Moreover, the cytotoxicity of XWL-1-48 is more potent than its congener GL331 and the IC(50) values are from 0.34 0.21 to 3.54 0.54 M …
Podophyllotoxin derivatives: a patent review (2012 - 2014).
Kamal A, Ali Hussaini SM, Rahim A, Riyaz S. Kamal A, et al. Expert Opin Ther Pat. 2015;25(9):1025-34. doi: 10.1517/13543776.2015.1051727. Epub 2015 Jun 2. Expert Opin Ther Pat. 2015. PMID: 26027947 Review.
EXPERT OPINION: After the successful development of etoposide and teniposide there has been considerable interest in the PPT skeleton to develop newer chemotherapeutic agents. In this regard, several PPT derivatives such as TOP53, GL331, NK611, F11782, and so on, have been …
EXPERT OPINION: After the successful development of etoposide and teniposide there has been considerable interest in the PPT skeleton to dev …
Recent progress on C-4-modified podophyllotoxin analogs as potent antitumor agents.
Liu YQ, Tian J, Qian K, Zhao XB, Morris-Natschke SL, Yang L, Nan X, Tian X, Lee KH. Liu YQ, et al. Med Res Rev. 2015 Jan;35(1):1-62. doi: 10.1002/med.21319. Epub 2014 May 14. Med Res Rev. 2015. PMID: 24827545 Free PMC article. Review.
Accordingly, numerous PPT derivatives have been prepared via hemisynthesis and important structure-activity relationship (SAR) correlations have been identified. Several resulting compounds, including GL-331, TOP-53, and NK611, reached clinical trials. Some excellen …
Accordingly, numerous PPT derivatives have been prepared via hemisynthesis and important structure-activity relationship (SAR) correlations …
Induction of cell cycle arrest by GL331 via triggering an ATM-dependent DNA damage response in HepG2 cells.
Wang YJ, Chen XG, Xiao ZY, Liu GT, Sun H. Wang YJ, et al. J Asian Nat Prod Res. 2012;14(7):657-64. doi: 10.1080/10286020.2012.684683. Epub 2012 May 15. J Asian Nat Prod Res. 2012. PMID: 22583615
GL331, a topoisomerase II inhibitor, has been found to trigger DNA damage response (DDR) to induce cell cycle arrest. ...As a result, GL331 could induce S arrest and up-regulate the phosphorylation of the histone H2AX variant (gamma-H2AX). ...
GL331, a topoisomerase II inhibitor, has been found to trigger DNA damage response (DDR) to induce cell cycle arrest. ...As a result, …
Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach.
Lee KH. Lee KH. J Nat Prod. 2010 Mar 26;73(3):500-16. doi: 10.1021/np900821e. J Nat Prod. 2010. PMID: 20187635 Free PMC article. Review.
Bevirimat is also the first in a new class of HIV drug candidates called "maturation inhibitors". In addition, an etoposide analogue, GL-331, progressed to anticancer phase II clinical trials, and the curcumin analogue JC-9 is in phase II clinical trials for treatin …
Bevirimat is also the first in a new class of HIV drug candidates called "maturation inhibitors". In addition, an etoposide analogue, GL …
[Mechanism of regulation of leptin expression in human lung adenocarcinoma cells by hypoxia inducible factor-1alpha: a preliminary study].
Zhang YB, Fang M, He FL, Hua TF, Hu BD, Zhao H, Liu RY. Zhang YB, et al. Zhonghua Yi Xue Za Zhi. 2008 Nov 4;88(40):2848-53. Zhonghua Yi Xue Za Zhi. 2008. PMID: 19080496 Chinese.
Human lung adenocarcinoma cells of the line A549 cells were cultured for 0, 12, 24, and 48 h respectively, exposed to hypoxia induced by CoCl2. Other A549 cells were treated with GL331, a kind of HIF-1alpha inhibitor, of the concentrations of 0, 5, 10, or 20 micromol/L und …
Human lung adenocarcinoma cells of the line A549 cells were cultured for 0, 12, 24, and 48 h respectively, exposed to hypoxia induced by CoC …
GL331, a topoisomerase II inhibitor, induces radiosensitization of human glioma cells.
Chen Y, Lin TY, Chen JC, Yang HZ, Tseng SH. Chen Y, et al. Anticancer Res. 2006 May-Jun;26(3A):2149-56. Anticancer Res. 2006. PMID: 16827158 Free article.
A combination treatment, using either concomitant irradiation at the beginning or end of the GL331 treatment (designated as the RT-GL331 and GL331-RT protocols, respectively), was used to investigate the radiosensitization effects of GL331. ...The comb …
A combination treatment, using either concomitant irradiation at the beginning or end of the GL331 treatment (designated as the RT- …
Induction of apoptosis and cell cycle arrest in glioma cells by GL331 (a topoisomerase II inhibitor).
Chen Y, Su YH, Wang CH, Wu JM, Chen JC, Tseng SH. Chen Y, et al. Anticancer Res. 2005 Nov-Dec;25(6B):4203-8. Anticancer Res. 2005. PMID: 16309217 Free article.
BACKGROUND: GL331 is a topoisomerase II inhibitor and, in this study, the effects of GL331 upon rat C6 glioma cells were investigated. MATERIALS AND METHODS: The glioma cells were treated with GL331, then a cytotoxicity assay was done to evaluate the cytotoxi …
BACKGROUND: GL331 is a topoisomerase II inhibitor and, in this study, the effects of GL331 upon rat C6 glioma cells were inves …
31 results