175203-55-1Relevant academic research and scientific papers
A new NT4 peptide-based drug delivery system for cancer treatment
Bracci, Luisa,Brunetti, Jlenia,Cipriani, Giulia,Depau, Lorenzo,Falciani, Chiara,Fragai, Marco,Menichetti, Stefano,Piantini, Sara,Pini, Alessandro,Scali, Silvia
, (2020/03/13)
The development of selective tumor targeting agents to deliver multiple units of chemotherapy drugs to cancer tissue would improve treatment efficacy and greatly advance progress in cancer therapy. Here we report a new drug delivery system based on a tetr
Synthesis and Electrochemical, Photophysical, and Self-Assembly Studies on Water-Soluble pH-Responsive Alkynylplatinum(II) Terpyridine Complexes
Chung, Clive Yik-Sham,Li, Steve Po-Yam,Lo, Kenneth Kam-Wing,Yam, Vivian Wing-Wah
, p. 4650 - 4663 (2016/05/24)
A series of water-soluble pH-responsive alkynylplatinum(II) terpyridine complexes have been synthesized and characterized. The electronic absorption, emission, and electrochemical properties of the complexes have been studied. The self-assembly processes of representative complexes in aqueous media, presumably through Pt?Pt and/or π-π interactions, have been investigated by concentration- and temperature-dependent UV-vis absorption measurements and dynamic light scattering experiments. Interestingly, some of the complexes have been found to undergo induced self-assembly and disassembly in aqueous media through modulation of the pH value of the solutions, resulting in remarkable UV-vis absorption and emission spectral changes. The emission spectral changes have been rationalized by the change in the hydrophilicity of the complexes, electrostatic repulsion among the complex molecules, and/or the extent of photoinduced electron transfer (PET) quenching upon protonation/deprotonation of the pH-responsive groups on the complexes. By simple modifications of the chemical structures of the complexes, induced self-assembly/disassembly of the complexes can occur at different and/or multiple pH regions, thus allowing the probing of changes at the desired pH region by triplet metal-metal-to-ligand charge-transfer emission of the complexes in the near-infrared (NIR) region. Fixed-cell imaging experiments have further demonstrated the potential of this class of complexes as pH-responsive NIR luminescent probes in vitro, while the NIR emissions of the complexes from live cells have been found to show good differentiation of acidic organelles such as lysosomes from other cellular compartments.
Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents
Zhang, Wenjuan,Li, Zhi,Zhou, Meng,Wu, Feng,Hou, Xueyan,Luo, Hao,Liu, Hao,Han, Xuan,Yan, Guoyi,Ding, Zhenyu,Li, Rui
supporting information, p. 799 - 807 (2014/02/14)
In this research, a series of 4-(1,2,3-triazol-1-yl)coumarin conjugates were synthesized and their anticancer activities were evaluated in vitro against three human cancer cell lines, including human breast carcinoma MCF-7 cell, colon carcinoma SW480 cell and lung carcinoma A549 cell. To increase the biological potency, structural optimization campaign was conducted focusing on the C-4 position of 1,2,3-triazole and the C-6, C-7 positions of coumarin. In addition, to further evaluate the role of 1,2,3-triazole and coumarin for antiproliferative activity, 9 compounds possessing 4-(piperazin-1-yl)coumarin framework and 3 derivatives baring quinoline core were also synthesized. By MTT assay in vitro, most of the compounds display attractive antitumor activities, especially 23. Further flow cytometry assays demonstrate that compound 23 exerts the antiproliferative role through arresting G2/M cell-cycle and inducing apoptosis.
Anticancer (hexacarbonyldicobalt)propargyl aryl ethers: Synthesis, antiproliferative activity, apoptosis induction, and effect on cellular oxidative stress
Schimler, Sydonie D.,Hall, David J.,Debbert, Stefan L.
, p. 28 - 37 (2013/02/25)
While an increasing number of (hexacarbonyldicobalt)alkynes have been found to possess antiproliferative activity against a number of cancer cell lines, the role of the organometallic moiety in this bioactivity is not well understood. To gain a better und
Hybrid system of metal/Bronsted acid relay catalysis for the intramolecular double hydroarylation and cationic cyclization of diyne diethers and diamines
Mo, Juntae,Eom, Dahan,Lee, Euichul,Lee, Phil Ho
supporting information; experimental part, p. 3684 - 3687 (2012/08/28)
We have developed a hybrid system of metal/Bronsted acid relay catalysis for the intramolecular double hydroarylation and cationic cyclization of diyne diethers and diamines to give 4,4′-bi(2H-chromene), bi(2H-quinoline), and dioxafluoranthenes starting f
Structure-based rational design of novel hit compounds for pyruvate dehydrogenase multienzyme complex E1 components from Escherichia coli
Ren, Yanliang,He, Junbo,Feng, Lingling,Liao, Xun,Jin, Jing,Li, Yongjian,Cao, Yi,Wan, Jian,He, Hongwu
experimental part, p. 7501 - 7506 (2012/01/03)
Pyruvate dehydrogenase multienzyme complex (PDHc) E1 component plays a pivotal role in cellular metabolism to convert the product of glycolysis (pyruvate) to acetyl-CoA, and has been reported as a potential target for anti-microbial and herbicide. In pres
Synthesis of symmetrical and unsymmetrical trisubstituted benzene derivatives through ring-closing alkyne metathesis strategy and dcpropargylation with various catalysts
Kotha, Sambasivarao,Bansal, Dccpti,Kumar, Ramanatham Vinod
scheme or table, p. 225 - 230 (2009/12/03)
Alkync trimerizalion by application of the Grubbs ruthenium first generation catalyst has been demonstrated. In this regard, triaryloxymethylbenzene derivatives have been generated by co- trimerization of propargylated phenol derivatives with the aid of the Grubbs catalyst. Depropargylation under various catalysts have been studied.
Design, synthesis and evaluation of monovalent ligands for the asialoglycoprotein receptor (ASGP-R)
Stokmaier, Daniela,Khorev, Oleg,Cutting, Brian,Born, Rita,Ricklin, Daniel,Ernst, Thomas O.G.,Boeni, Fabienne,Schwingruber, Kathrin,Gentner, Martin,Wittwer, Matthias,Spreafico, Morena,Vedani, Angelo,Rabbani, Said,Schwardt, Oliver,Ernst, Beat
experimental part, p. 7254 - 7264 (2010/03/24)
A series of novel aryl-substituted triazolyl d-galactosamine derivatives was synthesized as ligands for the carbohydrate recognition domain of the major subunit H1 (H1-CRD) of the human asialoglycoprotein receptor (ASGP-R). The compounds were biologically evaluated with a newly developed competitive binding assay, surface plasmon resonance and by a competitive NMR binding experiment. With compound 1b, a new ligand with a twofold improved affinity to the best so far known d-GalNAc was identified. This small, drug-like ligand can be used as targeting device for drug delivery to hepatocytes.
An efficient chemical approach to bispecific antibodies and antibodies of high valency
Gavrilyuk, Julia I.,Wuellner, Ulrich,Salahuddin, Syed,Goswami, Rajib K.,Sinha, Subhash C.,Barbas III, Carlos F.
supporting information; experimental part, p. 3716 - 3720 (2010/02/28)
Irreversible chemical programming of monoclonal aldolase antibody (mAb) 38C2 has been accomplished with β-lactam equipped mono- and bifunctional targeting modules, including a cyclic-RGD peptide linked to either the peptide (d-Lys6)-LHRH or ano
