67455-41-8Relevant articles and documents
Methylene violet derivative fluorescent probe as well as synthesis method and application thereof
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, (2021/03/13)
The invention discloses a methylene violet derivative fluorescent probe as well as a synthesis method and application thereof. The fluorescent probe is connected with an NBD group through piperazine on the basis of a cationic main structure of methylene violet. The preparation method comprises the following steps: directly reacting methylene violet 3RAX with piperazine, or firstly reacting with X-R5-X and then reacting with piperazine, and finally introducing an NBD group to a piperazine group to obtain the target fluorescent probe; or reacting 4-fluoronitrobenzene, piperazine and aniline to obtain a cationic main structure of methylene violet, and finally introducing an NBD group to a piperazine group to obtain the target fluorescent probe. The fluorescent probe is good in water solubility, can be used for sulfur ion detection, is high in detection sensitivity and low in detection limit, and can also be used as a tumor photodynamic therapy probe to quickly release singlet oxygen for tumor photodynamic therapy; synthesis is simple, conditions are mild, and cost is low.
Discovery and SARs of 5-Chloro- N4-phenyl- N2-(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors with Potent Antitumor Activity
Wang, Yang,Chen, Xing,Yan, Yaoyao,Zhu, Xiaochen,Liu, Mingming,Liu, Xinhua
, p. 3327 - 3347 (2020/04/08)
Cyclin-dependent kinases (CDKs) are promising therapeutic targets for cancer therapy. Herein, we describe our efforts toward the discovery of a series of 5-chloro-N4-phenyl-N2-(pyridin-2-yl)pyrimidine-2,4-diamine derivatives as dual CDK6 and 9 inhibitors. Intensive structural modifications lead to the identification of compound 66 as the most active dual CDK6/9 inhibitor with balancing potency against these two targets and good selectivity over CDK2. Further biological studies revealed that compound 66 was directly bound to CDK6/9, resulting in suppression of their downstream signaling pathway and inhibition of cell proliferation by blocking cell cycle progression and inducing cellular apoptosis. More importantly, compound 66 significantly inhibited tumor growth in a xenograft mouse model with no obvious toxicity, indicating the promising therapeutic potential of CDK6/9 dual inhibitors for cancer treatment. Therefore, the above results are of great importance in the development of dual CDK6/9 inhibitors for cancer therapy.
Method for reducing aromatic nitro compounds into aromatic amine compounds
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Paragraph 0028-0029, (2020/03/25)
The invention discloses a method for reducing aromatic nitro compounds into aromatic amine compounds. The aromatic nitro compounds are reacted at a temperature of 110-130 DEG C in an inert or air atmosphere under the action of a rhodium catalyst by using water as a solvent, isopropanol as a hydrogen source and potassium phosphate or sodium carbonate as an alkali to obtain the aromatic amine compounds. The method has the advantages of simplicity in operation, greenness, environmental friendliness, reduction of environmental pollution, high reaction yield, amplified gram-scale preparation of theamine compounds, high catalyst activity, recyclability and low industrial production cost.
