Design, synthesis and evaluation of a novel π–π stacking nano-intercalator as an anti-tumor agent

MedChemComm ◽  
2016 ◽  
Vol 7 (2) ◽  
pp. 247-257 ◽  
Author(s):  
Haimei Zhu ◽  
Yuanbo Song ◽  
Yuji Wang ◽  
Ming Zhao ◽  
Yi Ren ◽  
...  

A strategy for designing safe and effective π–π stacking nano-intercalators as anti-tumor agents was presented for the first time.

2022 ◽  
Author(s):  
Zhi-Gang Yin ◽  
Xiong-Wei Liu ◽  
Hui-Juan Wang ◽  
Min Zhang ◽  
Xiong-Li Liu ◽  
...  

A highly efficient synthesis of structurally diverse ortho-acylphenol–diindolylmethane hybrids 3 using carboxylic acid-activated chromones as versatile synthetic building blocks is reported here for the first time, through 1,4-nucleophilic addition and followed by a decarboxylation and pyrone ring opening reaction process.


2016 ◽  
Vol 7 (34) ◽  
pp. 5445-5455 ◽  
Author(s):  
Ming Yang ◽  
Dongxiong Mao ◽  
Sheng Chen ◽  
Hailiang Zhang

A reentrant phase is observed for the first time in dendronized polystyrenes with high molecular weight through regulating the length of tail chains.


MedChemComm ◽  
2019 ◽  
Vol 10 (4) ◽  
pp. 573-583 ◽  
Author(s):  
Runde Xiong ◽  
Dongxiu He ◽  
Xiangping Deng ◽  
Juan Liu ◽  
Xiaoyong Lei ◽  
...  

According to the combination principle, target compounds were designed, and compound E20 might be a promising anti-tumor agent targeting gastric cancer.


2017 ◽  
Vol 53 (68) ◽  
pp. 9438-9441 ◽  
Author(s):  
Xinyuan He ◽  
Yiming Hu ◽  
Wen Shi ◽  
Xiaohua Li ◽  
Huimin Ma

We have, for the first time, developed a near-infrared fluorescent probe for aminopeptidase N by combining a hemicyanine and an alanyl residue.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kavitha Kankanala ◽  
Vangala Ranga Reddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
Khagga Mukkanti ◽  
...  

The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.


2016 ◽  
Vol 45 (32) ◽  
pp. 12846-12853 ◽  
Author(s):  
Dieter Sorsche ◽  
Markus Schaub ◽  
Frank W. Heinemann ◽  
Johannes Habermehl ◽  
Susanne Kuhri ◽  
...  

Electrostatic repulsion between gold(iii) coordination spheres exceeds π-stacking for the first time in a tpphz-bridged dinuclear PMD model complex.


Author(s):  
Joël Gubler ◽  
Peter Chen

N-[(Z)-2-(2H-1,3,2-Benzodioxaborol-2-yl)-2-phenylethenyl]-N-(propan-2-yl)aniline, C23H22BNO2, contains a C=C bond that is conjugated with a donor and an acceptor group. An analysis that included similar push–pull olefins revealed that bond lengths in their B—C=C—N core units correlate with the perceived acceptor and donor strength of the groups. The two phenyl groups in the molecule are rotated with respect to the plane that contains the BCCN atoms, and are close enough for significant π-stacking. Definite characterization of the title compound demonstrates, for the first time in a reliable way, that hydroboration of ynamines with borandiol esters is feasible. Compared to olefin hydroboration with borane, the ynamine substrate is activated enough to undergo reaction with the less active hydroboration reagent catecholborane.


Oncogenesis ◽  
2019 ◽  
Vol 8 (12) ◽  
Author(s):  
Jiheng Xu ◽  
Xiaohui Hua ◽  
Rui Yang ◽  
Honglei Jin ◽  
Jingxia Li ◽  
...  

AbstractXIAP has generally been thought to function in bladder cancer. However, the potential function of structure-based function of XIAP in human BC invasion has not been well explored before. We show here that ectopic expression of the BIR domains of XIAP specifically resulted in MMP2 activation and cell invasion in XIAP-deleted BC cells, while Src was further defined as an XIAP downstream negative regulator for MMP2 activation and BC cell invasion. The inhibition of Src expression by the BIR domains was caused by attenuation of Src protein translation upon miR-203 upregulation; which was resulted from direct interaction of BIR2 and BIR3 with E2F1 and Sp1, respectively. The interaction of BIR2/BIR3 with E2F1/Sp1 unexpectedly occurred, which could be blocked by serum-induced XIAP translocation. Taken together, our studies, for the first time revealed that: (1) BIR2 and BIR3 domains of XIAP play their role in cancer cell invasion without affecting cell migration by specific activation of MMP2 in human BC cells; (2) by BIR2 interacting with E2F1 and BIR3 interacting with Sp1, XIAP initiates E2F1/Sp1 positive feedback loop-dependent transcription of miR-203, which in turn inhibits Src protein translation, further leading to MMP2-cleaved activation; (3) XIAP interaction with E2F1 and Sp1 is observed in the nucleus. Our findings provide novel insights into understanding the specific function of BIR2 and BIR3 of XIAP in BC invasion, which will be highly significant for the design/synthesis of new BIR2/BIR3-based compounds for invasive BC treatment.


2020 ◽  
Vol 49 (4) ◽  
pp. 1109-1143 ◽  
Author(s):  
Zhichao Zeng ◽  
Yueshan Xu ◽  
Zheshan Zhang ◽  
Zhansheng Gao ◽  
Meng Luo ◽  
...  

Rare-earth-containing halide and oxide perovskite nanomaterials are systematically reviewed for the first time, providing interdisciplinary challenges and opportunities to researchers.


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