The Experts below are selected from a list of 3705 Experts worldwide ranked by ideXlab platform
Mohamed Akssira - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and anticancer evaluation of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
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Synthesis and anticancer evaluation of novel 9α-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed A. Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
Lianxiang Luo - One of the best experts on this subject based on the ideXlab platform.
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Parthenolide inhibits the growth of non small cell lung cancer by targeting epidermal growth factor receptor
Cancer Cell International, 2020Co-Authors: Riming Huang, Zheng Zhu, Zhiyan Chen, Liao Cui, Hui Luo, Lianxiang LuoAbstract:EGFR tyrosine kinase inhibitors (TKIs) have been developed for the treatment of EGFR mutated NSCLC. Parthenolide, a natural product of Parthenolide, which belongs to the sesquiterpene lactone family and has a variety of biological and therapeutic activities, including anti-cancer effects. However, its effect on non-small cell lung cancer is little known. The CCK8 assay and colony formation assays were used to assess cell viability. Flow cytometry was used to measure the cell apoptosis. In silico molecular docking was used to evaluate the binding of Parthenolide to EGFR. Network pharmacology analysis was was used to evaluate the key gene of Parthenolide target NSCLC. Western blotting was used to evaluate the key proteins involved apoptosis and EGFR signalling. The effect of Parthenolide treatment in vivo was determined by using a xenograft mouse model. In this study, Parthenolide could induce apoptosis and growth inhibition in the EGFR mutated lung cancer cells. Parthenolide also reduces the phosphorylation of EGFR as well as its downstream signaling pathways MAPK/ERK and PI3K/Akt. Molecular docking analysis of EGFR binding site with Parthenolide show that the anti-cancer effect of Parthenolide against NSCLC is mediated by a strong binding to EGFR. Network pharmacology analysis show Parthenolide suppresses NSCLC via inhibition of EGFR expression. In addition, Parthenolide inhibits the growth of H1975 xenografts in nude mice, which is associated with the inhibition of the EGFR signaling pathway. Taken together, these results demonstrate effective inhibition of Parthenolide in NSCLC cell growth by targeting EGFR through downregulation of ERK and AKT expression, which could be promisingly used for patients carrying the EGFR mutation.
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Parthenolide inhibits the growth of non-small cell lung cancer by targeting epidermal growth factor receptor
2020Co-Authors: Riming Huang, Zheng Zhu, Zhiyan Chen, Liao Cui, Hui Luo, Lianxiang LuoAbstract:Abstract Background: EGFR tyrosine kinase inhibitors (TKIs) have been developed for the treatment of EGFR mutated NSCLC. Parthenolide, a natural product of Parthenolide, which belongs to the sesquiterpene lactone family and has a variety of biological and therapeutic activities, including anti-cancer effects. However, its effect on non-small cell lung cancer is little known. Methods: The CCK‑8 assay and colony formation assays were used to assess cell viability. Flow cytometry was used to measure the cell apoptosis. In silico molecular docking was used to evaluate the binding of Parthenolide to EGFR. Network pharmacology analysis was was used to evaluate the key gene of Parthenolide target NSCLC. Western blotting was used to evaluate the key proteins involved apoptosis and EGFR signalling. The effect of Parthenolide treatment in vivo was determined by using a xenograft mouse model.Results: In this study, Parthenolide could induce apoptosis and growth inhibition in the EGFR mutated lung cancer cells. Parthenolide also reduces the phosphorylation of EGFR as well as its downstream signaling pathways MAPK/ERK and PI3K/Akt. Molecular docking analysis of EGFR binding site with Parthenolide show that the anti-cancer effect of Parthenolide against NSCLC is mediated by a strong binding to EGFR. Network pharmacology analysis show Parthenolide suppresses NSCLC via inhibition of EGFR expression. In addition, Parthenolide inhibits the growth of H1975 xenografts in nude mice, which is associated with the inhibition of the EGFR signaling pathway. Conclusions: Taken together, these results demonstrate effective inhibition of Parthenolide in NSCLC cell growth by targeting EGFR through downregulation of ERK and AKT expression, which could be promisingly used for patients carrying the EGFR mutation.
Gerald Guillaumet - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and anticancer evaluation of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
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Synthesis and anticancer evaluation of novel 9α-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed A. Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
Abderrahman El Bouakher - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and anticancer evaluation of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
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Synthesis and anticancer evaluation of novel 9α-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed A. Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
Richard Daniellou - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and anticancer evaluation of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.
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Synthesis and anticancer evaluation of novel 9α-substituted-13-(1,2,3-triazolo)-Parthenolides
Tetrahedron Letters, 2016Co-Authors: Mohamed A. Zaki, Hassan Allouchi, Abderrahman El Bouakher, Eric Duverger, Ahmed El Hakmaoui, Richard Daniellou, Gerald Guillaumet, Mohamed AkssiraAbstract:A series of novel 9 alpha-substituted-13-(1,2,3-triazolo)-Parthenolides 3-20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9 alpha-Substituted-13-(1,2,3-triazolo)-Parthenolide derivatives were prepared by the diastereoselective Michael addition of TMSN3 onto 9 alpha-hydroxyParthenolide 1 to give the key intermediate 9 alpha-trimethylsilyloxy-13-(1,2,3-triazolo)-Parthenolide 2 which was utilized in a regioselective Huisgen 1,3-dipolar cycloaddition reaction with various alkynes to afford 1,4-disubstituted-1,2,3-triazoles of 9 alpha-substituted-Parthenolide. (C) 2016 Elsevier Ltd. All rights reserved.