1132-40-7Relevant articles and documents
Design and synthesis of 3-substituted indolin-2-one derivatives with methyl (e)-2-(3-Methoxy) acrylate moiety
Luo, Xi,Zhang, Yi-Ying,Wang, Yu-Liang
, p. 2911 - 2916 (2015)
In this article, fifteen indolin-2-one derivatives with methyl (E)-2-(3-methoxy)acrylate group were designed and synthesized. The structures of target compounds were confirmed by 1H NMR, IR and HR-MS spectra analysis.
The mechanism of Sandmeyer's cyclization reaction by electrospray ionization mass spectrometry
Silva, Barbara V.,Violante, Flavio A.,Pinto, Angelo C.,Santos, Leonardo S.
, p. 423 - 428 (2011)
Using electrospray ionization (tandem) mass spectrometry (ESI-MS(/MS)) spectrometric experiments, the Sandmeyer reaction was monitored on-line, and key intermediates were intercepted and characterized for the first time. The mechanistic information provided by on-line ESI-MS(/MS) is in accordance with Sandmeyer's proposal, and was made possible by coupling a microreactor on-line to the ESI ion source, which allowed reactions to be screened from 0.7-2.0 s, identifying and characterizing all intermediates that were formed and consumed during the reaction. Copyright
Microwave assisted preparation of isatins and synthesis of (±)- convolutamydine-A
Jnaneshwara,Bedekar,Deshpande
, p. 3627 - 3633 (1999)
Microwave assisted preparation of a number of isatin derivatives is reported. A simple synthesis of (±)-convolutamydine-A, a potent compound against leukemia cells, is presented.
A cinchona alkaloid catalyzed enantioselective sulfa-Michael/aldol cascade reaction of isoindigos: Construction of chiral bispirooxindole tetrahydrothiophenes with vicinal quaternary spirocenters
Gui, Yong-Yuan,Yang, Jian,Qi, Liang-Wen,Wang, Xiao,Tian, Fang,Li, Xiao-Nian,Peng, Lin,Wang, Li-Xin
, p. 6371 - 6379 (2015)
A cinchona alkaloid catalyzed diastereoselective and enantioselective sulfa-Michael/aldol cascade reaction between 1,4-dithiane-2,5-diol and isoindigos has been successfully developed to afford the highly congested bispirooxindole tetrahydrothiophenes with vicinal quaternary spirocenters in high yields (up to 91%), excellent diastereoselectivities (up to >20 : 1 dr), and good enantioselectivities (up to 98% ee). Some synthetic transformations of the reaction products were also studied.
Discovery of di-indolinone as a novel scaffold for protein tyrosine phosphatase 1B inhibitors
Dai, Hou-Ling,Gao, Li-Xin,Yang, Ying,Li, Jing-Ya,Cheng, Jia-Gao,Li, Jia,Wen, Ren,Peng, Yan-Qing,Zheng, Jian-Bin
, p. 7440 - 7443 (2012)
A series of di-indolinone derivatives was designed and synthesized to optimize our lead compounds basing on molecular docking study as PTP1B inhibitors. Successive enzymatic assay identified the synthetic di-indolinone as novel PTP1B inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other tested homologous PTPs.
Bicyclic heteroaryl compound with PAR4 antagonistic activity and application thereof
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Paragraph 0074-0077, (2020/08/02)
The invention discloses a bicyclic heteroaryl compound with PAR4 antagonistic activity and application thereof. The invention provides the bicyclic heteroaryl compound with PAR4 antagonistic activity,and the bicyclic heteroaryl compound has remarkable antagonistic activity on PAR4 in an in-vitro anti-platelet aggregation experiment, so that platelet aggregation is effectively inhibited, and the bicyclic heteroaryl compound can be used for preparing medicines for preventing or treating various thromboembolic diseases.
Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis
Aneja, Babita,Khan, Nashrah Sharif,Khan, Parvez,Queen, Aarfa,Hussain, Afzal,Rehman, Md. Tabish,Alajmi, Mohamed F.,El-Seedi, Hesham R.,Ali, Sher,Hassan, Md. Imtaiyaz,Abid, Mohammad
, p. 840 - 852 (2019/01/04)
Microtubule affinity-regulating kinase 4 (MARK4) is a potential drug target as the same is found to be over expressed in several types of cancers. In search of effective MARK4 inhibitors, we have synthesized and characterized Isatin-triazole hydrazones (9a-i) and evaluated their inhibitory potential. Of all the compounds, 9g showed better binding affinity and enzyme inhibition potential in sub micromolar range. Human serum albumin (HSA) binding assay suggested an easy transportation of 9g in blood stream due to its binding affinity. In vitro anticancer studies performed on MCF-7, MDA-MB-435s and HepG2 cells using 9g showed inhibition of cell proliferation and cell migration. Further, 9g induces apoptosis in these cancerous cells, with IC50 values of 6.22, 9.94 and 8.14 μM, respectively. Putatively, 9g seems to cause oxidative stress resulting in apoptosis. Functional assay of 9g with a panel of 26 kinases showed MARK4 specific profile. In conclusion, 9g seems to possess an effective inhibitory potential towards MARK4 adding an additional repertoire to anticancer therapeutics.