scholarly journals Design, synthesis and application in biological imaging of a novel red fluorescent dye based on a rhodanine derivative

RSC Advances ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 160-163
Author(s):  
Zijing Li ◽  
Bin Huang ◽  
Yuan Wang ◽  
Wenbo Yuan ◽  
Yijing Wu ◽  
...  

2RDNTPA can be applied in fluorescence imaging of living cancer cells (HepG2) with red emission of 620 nm and negligible cytotoxicity with a half maximal inhibitory concentration much more than 100 μM.

2018 ◽  
Vol 5 (12) ◽  
pp. 3061-3066 ◽  
Author(s):  
Mengliang Zhu ◽  
Chaorui Su ◽  
Peipei Xing ◽  
Yabin Zhou ◽  
Lei Gong ◽  
...  

A FRET based AceDAN–porphyrin(Zn) dyad was designed to generate red emission and singlet oxygen (1O2) simultaneously, which were utilized successfully for two-photon excited fluorescence imaging and PDT of cancer cells.


2003 ◽  
Vol 773 ◽  
Author(s):  
Xiaohu Gao ◽  
Shuming Nie ◽  
Wallace H. Coulter

AbstractLuminescent quantum dots (QDs) are emerging as a new class of biological labels with unique properties and applications that are not available from traditional organic dyes and fluorescent proteins. Here we report new developments in using semiconductor quantum dots for quantitative imaging and spectroscopy of single cancer cells. We show that both live and fixed cells can be labeled with multicolor QDs, and that single cells can be analyzed by fluorescence imaging and wavelength-resolved spectroscopy. These results raise new possibilities in cancer imaging, molecular profiling, and disease staging.


2020 ◽  
Vol 17 (11) ◽  
pp. 1330-1341
Author(s):  
Yan Zhang ◽  
Niefang Yu

Background: Fibroblast growth factors (FGFs) and their high affinity receptors (FGFRs) play a major role in cell proliferation, differentiation, migration, and apoptosis. Aberrant FGFR signaling pathway might accelerate development in a broad panel of malignant solid tumors. However, the full application of most existing small molecule FGFR inhibitors has become a challenge due to the potential target mutation. Hence, it has attracted a great deal of attention from both academic and industrial fields for hunting for novel FGFR inhibitors with potent inhibitory activities and high selectivity. Objective: Novel 5-amino-1H-pyrazole-1-carbonyl derivatives were designed, synthesized, and evaluated as FGFR inhibitors. Methods: A series of 5-amino-1H-pyrazole-1-carbonyl derivatives were established by a condensation of the suitable formyl acetonitrile derivatives with either hydrazine or hydrazide derivatives in the presence of anhydrous ethanol or toluene. The inhibitory activities of the target compounds were screened against the FGFRs and two representative cancer cell lines. Tests were carried out to observe the inhibition of 8e against FGFR phosphorylation and downstream signal phosphorylation in human gastric cancer cell lines (SNU-16). The molecular docking of all the compounds were performed using Molecular Operating Environment in order to evaluate their binding abilities with the corresponding protein kinase. Results: A series of 5-amino-1H-pyrazole-1-carbonyl derivatives have been designed and synthesized, screened for their inhibitory activities against FGFRs and cancer cell lines. Most of the target compounds showed moderate to good anti-proliferate activities against the tested enzymes and cell lines. The most promising compounds 8e suppressed FGFR1-3 with IC50 values of 56.4, 35.2, 95.5 nM, and potently inhibited the SNU-16 and MCF-7 cancer cells with IC50 values of 0.71 1.26 μM, respectively. And 8e inhibited the growth of cancer cells containing FGFR activated by multiple mechanisms. In addition, the binding interactions were quite similar in the molecular models between generated compounds and Debio-1347 with the FGFR1. Conclusion: According to the experimental findings, 5-amino-1H-pyrazole-1-carbonyl might serve as a promising template of an FGFR inhibitor.


2019 ◽  
Vol 18 (15) ◽  
pp. 2124-2130
Author(s):  
Amany Belal

Background: For further exploration of the promising pyrrolizine scaffold and in continuation of our previous work, that proved the potential anticancer activity of the hit compound I, a new series of pyrrolizines 2-5 and 7-9 were designed and synthesized. Methods: Structures of the new compounds were confirmed by IR, 1H-NMR, 13C-NMR and elemental analysis. Antitumor activity for the prepared compounds against human breast adenocarcinoma (MCF-7), liver (HEPG2) and colon (HCT116) cancer cell lines was evaluated using SRB assay method. Result: Compounds 2, 3 and 5 were the most potent on colon cancer cells, their IC50 values were less than 5 µM. Compounds 2, 3 and 8 were the most potent on liver cancer cells, their IC50 values were less than 10 µM. As for MCF7, compounds 2, 7, 8 and 9 were the most active with IC50 values less than 10 µM. We can conclude that combining pyrrolizine scaffold with urea gave abroad spectrum anticancer agent 2 against the three tested cell lines. Micronucleus assays showed that compounds 2, 3, 8 are mutagenic and can induce apoptosis. In addition, caspase-3 activation was evaluated and compound 2 showed increase in the level of caspase-3 (9 folds) followed by 3 (8.28 folds) then 8 (7.89 folds). Conclusion: The obtained results encourage considering these three compounds as novel anticancer prototypes.


RSC Advances ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 2656-2663
Author(s):  
Boye Zhang ◽  
Qianqian Duan ◽  
Yi Li ◽  
Jianming Wang ◽  
Wendong Zhang ◽  
...  

The system is pH-responsive and redox-controlled release. And the charge reversal and size transitions of the system can enhance the targeted ability. Moreover, the system can recognize the cancer cells by the fluorescence imaging.


Sensors ◽  
2017 ◽  
Vol 17 (12) ◽  
pp. 2942 ◽  
Author(s):  
Shota Izumi ◽  
Shohei Yamamura ◽  
Naoko Hayashi ◽  
Mana Toma ◽  
Keiko Tawa

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