5345-46-0Relevant articles and documents
Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone-Naphthalimide-Polyamine Conjugates with Antimetastatic Activity
Dai, Fujun,Li, Qian,Wang, Yuxia,Ge, Chaochao,Feng, Chenyang,Xie, Songqiang,He, Haoying,Xu, Xiaojuan,Wang, Chaojie
, p. 2071 - 2083 (2017)
Approximately 90% of cancer-associated deaths result from disseminated tumors, indicating the ineffectiveness of current therapies and the imperative need of antimetastatic drugs. A novel pharmacophore with flavonoid and naphthalimide moieties was constructed by using a fragment-based drug design and a series of eight flavone-naphthalimide-polyamine conjugates were synthesized. In vitro evaluation revealed that compound 6c with a homospermidine motif displayed better cell selectivity between cancerous and normal liver cells than amonafide did. The in vivo assays on two hepatocellular carcinoma (HCC) models verified that 6c potently suppressed pulmonary metastasis with improved organ indexes compared to amonafide. Various experiments showed that 6c as a potential fluorescent chemical probe could target the mitochondria. Preliminary investigation into the mechanism of action of 6c indicated that it might harness a polyamine transporter for cell entrance, localize in the mitochondria, selectively cause reactive oxygen species (ROS) overproduction in hepatoma cells instead of normal liver cells, and finally lead to HCC cell apoptosis and migration inhibition via multiple ROS-mediated signaling pathways.
A reactive cysteine probe and its preparation method (by machine translation)
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Paragraph 0041; 0042; 0045, (2017/08/31)
The invention discloses a reactive cysteine probe and its preparation method, in order to rhodamine derivative is a fluorophore, acrylic ester structure is a cysteine specific reactive group; probe itself fluorescence is extremely weak, strong fluorescent after reaction with cysteine, can be used for detection of the cysteine. The probe in PBS 7.4 (30% ethanol) system in half-cystine reaction is more rapid, has good selectivity and higher sensitivity; can be used to determine in biological and environmental system of the cysteine content of the fluorescence detection, visual qualitative detection, cell imaging detection. (by machine translation)
Reactive sulfhydryl compound probe and preparation method thereof
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Paragraph 0045; 0050; 0051, (2017/10/25)
The invention discloses a reactive sulfhydryl compound probe and a preparation method of the probe. A sensing molecule releases a rhodamine dye molecule monomer based on a thiol participated disulfide bond cleavage reaction, the fluorescence intensity is significantly improved, an obvious color change is accompanied, and selected interfering ions and the like almost have no influence on a detection effect, so that specific recognition response to a sulfhydryl compound is realized, and a detection limit reaches 0.124 micrometers.