7314-07-0Relevant academic research and scientific papers
Discovery of styrylaniline derivatives as novel alpha-synuclein aggregates ligands
Bian, Jiang,Liu, Yi-Qi,He, Jie,Lin, Xin,Qiu, Chen-Yang,Yu, Wen-Bo,Shen, Yan,Zhu, Ze-Yun,Ye, De-Yong,Wang, Jian,Chu, Yong
, (2021/10/06)
Parkinson's disease (PD) is the second most common neurodegenerative disorder. Early diagnosis is the key to treatment but is still a great challenge in the clinic now. The discovery of alpha-synuclein (α-syn) aggregates ligands has become an attractive s
TARGETED ABERRANT ALPHA-SYNUCLEIN SPECIES AND INDUCED UBIQUITINATION AND PROTEOSOMAL CLEARANCE VIA CO-RECRUITMENT OF AN E3-LIGASE SYSTEM
-
, (2022/02/06)
Disclosed are bispecific compounds (degraders) that target α-synuclein protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative diseases.
Xanthate-mediated synthesis of (E)-alkenes by semi-hydrogenation of alkynes using water as the hydrogen donor
Luo, Xianglin,Chen, Xiuwen,Chen, Lu,Zhang, Kun,Li, Yibiao
supporting information, p. 2170 - 2173 (2019/02/24)
Semi-hydrogenation of alkynes is one of the most widely used methods for obtaining alkenes in laboratory preparation and in industry. Transition metal catalysts have been extensively studied for this transformation, but the tolerance of functional groups, such as pyridine,-OH,-NH2,-Bpin, and halides, and the toxicity of the trace amount of transition metal catalysts are still highly challenging. In this study, we report a general and robust strategy to achieve the semi-hydrogenation of alkynes using inexpensive and commercially available xanthate as the mediator. Mechanism studies support a non-radical process and H2O acts as the hydrogen donor.
Discovery of efficient stimulators for adult hippocampal neurogenesis based on scaffolds in dragon's blood
Liang, Jian-Hua,Yang, Liang,Wu, Si,Liu, Si-Si,Cushman, Mark,Tian, Jing,Li, Nuo-Min,Yang, Qing-Hu,Zhang, He-Ao,Qiu, Yun-Jie,Xiang, Lin,Ma, Cong-Xuan,Li, Xue-Meng,Qing, Hong
supporting information, p. 382 - 392 (2017/05/19)
Reduction of hippocampal neurogenesis caused by aging and neurological disorders would impair neural circuits and result in memory loss. A new lead compound (N-trans-3′,4'-methylenedioxystilben-4-yl acetamide 27) has been discovered to efficiently stimulate adult rats' neurogenesis. In-depth structure-activity relationship studies proved the necessity of a stilbene scaffold that is absent in highly cytotoxic analogs such as chalcones and heteroaryl rings and inactive analogs such as diphenyl acetylene and diphenyl ethane, and validated the importance of an NH in the carboxamide and a methylenedioxy substituent on the benzene ring. Immunohistochemical staining and biochemical analysis indicate, in contrast to previously reported neuroprotective chemicals, N-stilbenyl carboxamides have extra capacity for neuroproliferation-type neurogenesis, thereby providing a foundation for improving the plasticity of the adult mammalian brain.
Synthesis and anticancer activity of new azo compounds containing extended π-conjugated systems
Rezaei-Seresht, Esmail,Mireskandari, Erfan,Kheirabadi, Mitra,Cheshomi, Hamid,Rezaei-Seresht, Hasan,Aldaghi, Leila Sadat
, p. 1463 - 1469 (2017/07/25)
A series of novel azo compounds with extended π-conjugated systems were prepared by azo coupling reaction compounds trans-2-(4′-aminostyryl)-thiophene, 1-(4-aminophenyl)-4-phenyl-1,3-butadiene and 4-amino-4′-methoxystilbene with some phenols. The compounds were evaluated for their cytotoxicity against breast cancer adenocarcinoma (MCF-7), cervix adenocarcinoma (HeLa) and human embryonic kidney (HEK 293) cell lines using the MTT assay. The results showed all derivatives had more toxic effects than tamoxifen. Of all the compounds tested, the azo product obtained from coupling trans-2-(4′-Aminostyryl)-thiophene with 2-naphthol (compound 5b) exhibited the potent in vitro antiproliferative activity with IC50 27 ± 1 and 18 ± 0 μg/mL against MCF-7 and HeLa cell lines, respectively, while it was devoid of any cytotoxicity against normal HEK 293 cells even at 200 μg/mL.
Inhibitory effect of cytotoxic stilbenes related to resveratrol on the expression of the VEGF, hTERT and c-Myc genes
Martí-Centelles, Rosa,Falomir, Eva,Murga, Juan,Carda, Miguel,Marco, J. Alberto
supporting information, p. 488 - 496 (2015/10/05)
A group of thirty-nine stilbene derivatives, prepared by means of Heck coupling reactions, has been investigated for their cytotoxicity, as well as for their ability to inhibit the production of the vascular endothelial growth factor (VEGF) and the activation of telomerase. The ability of these compounds to inhibit proliferation of two tumoral cell lines (HT-29 and MCF-7) and one non tumoral cell line (HEK-293) was first determined. Subsequently, we determined the capacity of the compounds to inhibit the secretion of VEGF in the aforementioned cell lines and to downregulate the expression of the VEGF, hTERT and c-Myc genes, the two latter involved in the control of the activation of telomerase. One of the synthetic stilbenes, (E)-4-(4-methoxystyryl)aniline, showed strong cytotoxicity and proved able to cause a marked decrease both in the secretion of VEGF and in the expression of the hTERT and c-Myc genes, in all cases at concentrations in the low nanomolar range.
Novel photochrome aptamer switch assay (PHASA) for adaptive binding to aptamers
Papper, Vladislav,Pokholenko, Oleksandr,Wu, Yuanyuan,Zhou, Yubin,Jianfeng, Ping,Steele, Terry W. J.,Marks, Robert S.
, p. 1581 - 1591 (2015/02/19)
A novel Photochrome-Aptamer Switch Assay (PHASA) for the detection and quantification of small environmentally important molecules such as toxins, explosives, drugs and pollutants, which are difficult to detect using antibodies-based assays with high sensitivity and specificity, has been developed. The assay is based on the conjugation of a particular stilbene-analyte derivative to any aptamer of interest. A unique feature of the stilbene molecule is its reporting power via trans-cis photoisomerisation (from fluorescent trans-isomer to non-fluorescent cis-isomer) upon irradiation with the excitation light. The resulting fluorescence decay rate for the trans-isomer of the stilbene-analyte depends on viscosity and spatial freedom to rotate in the surrounding medium and can be used to indicate the presence of the analyte. Quantification of the assay is achieved by calibration of the fluorescence decay rate for the amount of the tested analyte. Two different formats of PHASA have been recently developed: direct conjugation and adaptive binding. New stilbene-maleimide derivatives used in the adaptive binding format have been prepared and characterised. They demonstrate effective binding to the model thiol compound and to the thiolated Malachite Green aptamer.
Synthesis and bioactivity of resveratrol analogues
Ao, Junli,Chen, Yuanmou,Xu, Xiaoling,Zhang, Xu,Yu, Yue,Yu, Peng,Hua, Erbing
, p. 2092 - 2098 (2014/06/09)
It has been reported that resveratrol enhanced SIRT1 expression and significantly mimicked calorie restriction by stimulating Sir2 which is the most homologic homologue of SIRT1 of mammalian. A series of novel resveratrol derivatives were designed and synthesized as novel SIRT1 activator candidates. These synthesized compounds were characterized by spectral (1H NMR) analysis and examined for their Sir2 activation against yeast parental strain-BY4743 at a concentration of 100 μM/L by Bioscreen C MBR machine. Several compounds showed a promising Sir2 activation activity compared with resveratrol. Meanwhile, the structure-activity relationships with Sirt2 activation activities were also discussed.
Design, synthesis, and evaluation of multitarget-directed resveratrol derivatives for the treatment of Alzheimer's disease
Lu, Chuanjun,Guo, Yueyan,Yan, Jun,Luo, Zonghua,Luo, Hai-Bin,Yan, Ming,Huang, Ling,Li, Xingshu
, p. 5843 - 5859 (2013/08/23)
A series of multitarget-directed resveratrol derivatives was designed and synthesized for the treatment of Alzheimer's disease (AD). In vitro studies indicated that most of the target compounds exhibit significant inhibition of self-induced β-amyloid (Aβ)
Substituent effects on the 13C NMR chemical shifts of the imine carbon in N-(4-X-benzylidene)-4-(4-Y-styryl) anilines
Fang, Zhengjun,Cao, Chenzhong,Chen, Guanfan
, p. 1343 - 1350 (2013/08/24)
Long-range electronic substituent effects were targeted using the substituent dependence of δC(C=N), and specific cross-interactions were explored extendedly. A wide set of N-(4-X-benzylidene)- 4-(4-Y-styryl) anilines, p-X-C6H4
