33284-00-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells
He, Zhang-Xu,Huo, Jin-Ling,Gong, Yun-Peng,An, Qi,Zhang, Xin,Qiao, Hui,Yang, Fei-Fei,Zhang, Xin-Hui,Jiao, Le-Min,Liu, Hong-Min,Ma, Li-Ying,Zhao, Wen
, (2020/11/24)
To discover novel anticancer agents with potent and low toxicity, we designed and synthesized a range of new thiosemicarbazone-indole analogues based on lead compound 4 we reported previously. Most compounds displayed moderate to high anticancer activities against five tested tumor cells (PC3, EC109, DU-145, MGC803, MCF-7). Specifically, the represented compound 16f possessed strong antiproliferative potency and high selectivity toward PC3 cells with the IC50 value of 0.054 μM, compared with normal WPMY-1 cells with the IC50 value of 19.470 μM. Preliminary mechanism research indicated that compound 16f could significantly suppress prostate cancer cells (PC3, DU-145) growth and colony formation in a dose-dependent manner. Besides, derivative 16f induced G1/S cycle arrest and apoptosis, which may be related to ROS accumulation due to the activation of MAPK signaling pathway. Furthermore, molecule 16f could effectively inhibit tumor growth through a xenograft model bearing PC3 cells and had no evident toxicity in vivo. Overall, based on the biological activity evaluation, analogue 16f can be viewed as a potential lead compound for further development of novel anti-prostate cancer drug.
Thiosemicarbazone derivative containing indole fragment, and preparation method and application thereof
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Paragraph 0276; 0280-0281, (2019/11/21)
The invention provides a thiosemicarbazone derivative containing an indole fragment, and a preparation method and application thereof, belonging to the technical field of medicinal chemistry. The invention provides the thiosemicarbazone derivative containing the indole fragment. The thiosemicarbazone derivative containing the indole fragment provided by the invention has strong cell proliferationinhibitory activity on PC3 cells and MGC803 cells, and shows smaller toxic and side effects on normal cells, thereby providing a basis for drug screening. In addition, the preparation method for the thiosemicarbazone derivative containing the indole fragment in the invention is simple in process, high in yield, and suitable for industrial production.
Optimization of rutaecarpine as ABCA1 up-regulator for treating atherosclerosis
Li, Yongzhen,Feng, Tingting,Liu, Peng,Liu, Chang,Wang, Xiao,Li, Dongsheng,Li, Ni,Chen, Minghua,Xu, Yanni,Si, Shuyi
supporting information, p. 884 - 888 (2014/09/17)
ATP-binding cassette transporter A1 (ABCA1) is a key transporter and receptor in promoting cholesterol efflux, and increasing the expression level of ABCA1 is antiatherogenic. In our previous study, rutaecarpine (RUT) was found to protect ApoE-/- mice from developing atherosclerosis through preferentially up-regulating ABCA1 expression. In the present work, a series of RUT derivatives were synthesized and examined as ABCA1 expression up-regulators. Compounds CD1, CD6, and BCD1-2 were found to possess the most potential activity as antiatherosclerotic agents among all compounds tested.
A biomolecule-compatible visible-light-induced azide reduction from a DNA-encoded reaction-discovery system
Chen, Yiyun,Kamlet, Adam S.,Steinman, Jonathan B.,Liu, David R.
experimental part, p. 146 - 153 (2012/02/17)
Using a system that accelerates the serendipitous discovery of new reactions by evaluating hundreds of DNA-encoded substrate combinations in a single experiment, we explored a broad range of reaction conditions for new bond-forming reactions. We discovered reactivity that led to a biomolecule-compatible, Ru(II)-catalysed azide-reduction reaction induced by visible light. In contrast to current azide-reduction methods, this reaction is highly chemoselective and is compatible with alcohols, phenols, acids, alkenes, alkynes, aldehydes, alkyl halides, alkyl mesylates and disulfides. The remarkable functional group compatibility and mild conditions of the reaction enabled the azide reduction of nucleic acid and oligosaccharide substrates, with no detectable occurrence of side reactions. The reaction was also performed in the presence of a protein enzyme without the loss of enzymatic activity, in contrast to two commonly used azide-reduction methods. The visible-light dependence of this reaction provides a means of photouncaging functional groups, such as amines and carboxylates, on biological macromolecules without using ultraviolet irradiation.
