A non-sulfur chemosensor based on an easy to prepare double naphthalene Schiff base is reported for the colorimetric and fluorometric dual-channel sensing of Hg2+ ions by taking advantage of the twisted intramolecular...A non-sulfur chemosensor based on an easy to prepare double naphthalene Schiff base is reported for the colorimetric and fluorometric dual-channel sensing of Hg2+ ions by taking advantage of the twisted intramolecular charge transfer (TICT) mechanism. This work provides a novel approach for the selective recognition of mercury ions. Moreover, this sensor serves as a potential recyclable component in sensing materials and the complex L-Hg2+ (L = 1-[(2-naphthalenylimino)methyl]-2-naphthalenol) can therefore be used as a fluorescent sensor for iodine anions. Notably, the color changes are very significant and all the recognition and recycling processes can be observed by the naked eye.展开更多
The mammalian target of rapamycin(mTOR) is a critical component of the PI3K-AKT signaling pathway. It is highly activated in cervical cancer, which continues to pose an important clinical challenge with an urgent need...The mammalian target of rapamycin(mTOR) is a critical component of the PI3K-AKT signaling pathway. It is highly activated in cervical cancer, which continues to pose an important clinical challenge with an urgent need for new and improved therapeutic approaches. Herein, we describe the structure-based drug discovery and biological evaluation of a series of m TOR kinase inhibitors as potential anti-cervical cancer agents. The results of enzymatic activity assays supported C3 as a potential m TOR inhibitor, which exhibited high inhibitory activity with an IC50 of 1.57 μM. Molecular docking and dynamics simulation were conducted to predict the binding patterns, suggesting relationships between structure and activity. The anti-proliferative assay against diverse cancer cell lines was displayed subsequently, revealing that C3 exhibited significant proliferation inhibition against cervical cancer cell He La(IC50=0.38μM) compared with other cell lines. Moreover, C3 could effectively reduce the expression of phospho-ribosomal S6 protein(p-S6) in He La cells in a dose-dependent manner. Noteworthily, m TOR signaling and other cellular pathways might contribute to the significant effect of C3 against cervical cancer simultaneously. These data indicated that C3 represented a good lead molecule for further development as a therapeutic agent for cervical cancer treatment.展开更多
基金supported by the National Natural Science Foundation of China (21064006, 21161018)the Natural Science Foundation of Gansu Province (1010RJZA018)the Program for Changjiang Scholars and Innovative Research Teams in Universities of the Ministry of Education of China (IRT1177)
文摘A non-sulfur chemosensor based on an easy to prepare double naphthalene Schiff base is reported for the colorimetric and fluorometric dual-channel sensing of Hg2+ ions by taking advantage of the twisted intramolecular charge transfer (TICT) mechanism. This work provides a novel approach for the selective recognition of mercury ions. Moreover, this sensor serves as a potential recyclable component in sensing materials and the complex L-Hg2+ (L = 1-[(2-naphthalenylimino)methyl]-2-naphthalenol) can therefore be used as a fluorescent sensor for iodine anions. Notably, the color changes are very significant and all the recognition and recycling processes can be observed by the naked eye.
基金National Natural Science Foundation of China(Grant No.21772005,81872730)the Beijing Natural Science Foundation(Grant No.7202088,7172118)。
文摘The mammalian target of rapamycin(mTOR) is a critical component of the PI3K-AKT signaling pathway. It is highly activated in cervical cancer, which continues to pose an important clinical challenge with an urgent need for new and improved therapeutic approaches. Herein, we describe the structure-based drug discovery and biological evaluation of a series of m TOR kinase inhibitors as potential anti-cervical cancer agents. The results of enzymatic activity assays supported C3 as a potential m TOR inhibitor, which exhibited high inhibitory activity with an IC50 of 1.57 μM. Molecular docking and dynamics simulation were conducted to predict the binding patterns, suggesting relationships between structure and activity. The anti-proliferative assay against diverse cancer cell lines was displayed subsequently, revealing that C3 exhibited significant proliferation inhibition against cervical cancer cell He La(IC50=0.38μM) compared with other cell lines. Moreover, C3 could effectively reduce the expression of phospho-ribosomal S6 protein(p-S6) in He La cells in a dose-dependent manner. Noteworthily, m TOR signaling and other cellular pathways might contribute to the significant effect of C3 against cervical cancer simultaneously. These data indicated that C3 represented a good lead molecule for further development as a therapeutic agent for cervical cancer treatment.
