5651-86-5Relevant articles and documents
Synthesis and chemical properties of conjugated polyacetylenes having pendant fullerene and/or porphyrin units
Lu, Fushen,Xiao, Shengqiang,Li, Yuliang,Liu, Huibiao,Li, Hongmei,Zhuang, Junpeng,Liu, Yang,Wang, Ning,He, Xiaorong,Li, Xiaofang,Gan, Liangbing,Zhu, Daoben
, p. 7444 - 7450 (2004)
Conjugated polyacetylenes having pendant fullerene and/or porphyrin groups were prepared by copolymerization in the presence of [Rh(nbd)Cl] 2-NEt3 in CHCl3. The photochemical and electrochemical properties of the polymers
Catalytic Modification of Dehydroalanine in Peptides and Proteins by Palladium-Mediated Cross-Coupling
de Bruijn, A. Dowine,Roelfes, Gerard
, p. 12728 - 12733 (2018)
Dehydroalanine (Dha) is a remarkably versatile non-canonical amino acid often found in antimicrobial peptides. Herein, we present the catalytic modification of Dha by a palladium-mediated cross-coupling reaction. By using Pd(EDTA)(OAc)2 as water-soluble catalyst, a variety of arylboronic acids was coupled to the dehydrated residues in proteins and peptides, such as Nisin. The cross-coupling reaction gave both the Heck product, in which the sp2-hybridisation of the α-carbon is retained, as well as the conjugated addition product. The reaction can be performed under mild aqueous conditions, which makes this method an attractive addition to the palette of bio-orthogonal catalytic methods.
An Efficient Approach for the Synthesis of 1,2,3-Triazole Moiety to Generate Uracil Molecular Architectures Through Cu-Catalyzed Azide–Alkyne Cycloaddition
Mohamed, Asmaa H.
, p. 2831 - 2838 (2019)
A simple and efficient pathway to tether conjugates of monosaccharides or aromatic moieties to uracil establishing a 1,2,3-triazole linker via click chemistry was reported. The reaction of arylimines of 5-amino uracil with propargyl bromide in a basic med
Tailor-made fluorescent trilobolide to study its biological relevance
Jurá?k, Michal,Rimpelová, Silvie,Kmoní?ková, Eva,Dra?ar, Pavel,Ruml, Tomá?
, p. 7947 - 7954 (2014)
Trilobolide (Tb) is a potent natural counterpart of thapsigargin, which has shown promising results in cancer clinical trials. Here, we report a rational approach to study intracellular localization and biological activity of this sesquiterpene lactone. We conjugated Tb with a green-emitting Bodipy dye attached by alternative linkers of different lengths. The live-cell imaging of the prepared bioconjugates brought clear evidence that Tb-Bodipy localized in the endoplasmic reticulum (ER) of various cancer cell lines. The localization signal was compared with ER-specific dyes. Cytotoxicity of Tb conjugates and impact on the mitochondrial physiology and nitric oxide release were also studied. The nitric oxide production and cytokine secretion in rat peritoneal cells indicate immunobiological potential of these lactone bioconjugates. In summary, our Tb-Bodipy conjugates could help us to reveal the molecular mechanism of trilobolide for its further potential use in biomedical applications.
Synthesis, docking and ADMET studies of novel chalcone triazoles for anti-cancer and anti-diabetic activity
Chinthala, Yakaiah,Thakur, Sneha,Tirunagari, Shalini,Chinde, Srinivas,Domatti, Anand Kumar,Arigari, Niranjana Kumar,Srinivas,Alam, Sarfaraz,Jonnala, Kotesh Kumar,Khan, Feroz,Tiwari, Ashok,Grover, Paramjit
, p. 564 - 573 (2015)
A series of novel chalcone-triazole derivatives were synthesized and screened for in vitro anticancer activity on the human cancer cell lines IMR32 (neuroblastoma), HepG2 (hepatoma) and MCF-7 (breast adenocarcinoma), DU-145 (prostate carcinoma), and A549
Just Add the Gold: Aggregation-Induced-Emission Properties of Alkynylphosphinegold(I) Complexes Functionalized with Phenylene-Terpyridine Subunits
Abramova, Evgenia O.,Paderina, Aleksandra V.,Slavova, Sofia O.,Kostenko, Ekaterina A.,Eliseenkov, Eugene V.,Petrovskii, Stanislav K.,Gitlina, Anastasia Yu.,Boyarskiy, Vadim P.,Grachova, Elena V.
supporting information, p. 18715 - 18725 (2021/12/09)
A series of organometallic complexes containing an alkynylphosphinegold(I) fragment and a phenylene-terpyridine moiety connected together by flexible linker have been prepared using the specially designed terpyridine ligands. The compounds were studied cr
Alkyne-tagged apigenin, a chemical tool to navigate potential targets of flavonoid anti-dengue leads
Badavath, Vishnu Nayak,Boonyasuppayakorn, Siwaporn,Chokmahasarn, Thamonwan,Hengphasatporn, Kowit,Jansongsaeng, Somruedee,Kaewmalai, Benyapa,Khotavivattana, Tanatorn,Rungrotmongkol, Thanyada,Saelee, Thanaphon,Shigeta, Yasuteru
, (2021/11/30)
A flavonoid is a versatile core structure with various cellular, immunological, and phar-macological effects. Recently, flavones have shown anti-dengue activities by interfering with viral translation and replication. However, the molecular target is still elusive. Here we chemically mod-ified apigenin by adding an alkyne moiety into the B-ring hydroxyl group. The alkyne serves as a chemical tag for the alkyne-azide cycloaddition reaction for subcellular visualization. The compound located at the perinuclear region at 1 and 6 h after infection. Interestingly, the compound signal started shifting to vesicle-like structures at 6 h and accumulated at 24 and 48 h after infection. Moreover, the compound treatment in dengue-infected cells showed that the compound restricted the viral protein inside the vesicles, especially at 48 h. As a result, the dengue envelope proteins spread throughout the cells. The alkyne-tagged apigenin showed a more potent efficacy at the EC50 of 2.36 ± 0.22, and 10.55 ± 3.37 μM, respectively, while the cytotoxicities were similar to the original apigenin at the CC50 of 70.34 ± 11.79, and 82.82 ± 11.68 μM, respectively. Molecular docking con-firmed the apigenin binding to the previously reported target, ribosomal protein S9, at two binding sites. The network analysis, homopharma, and molecular docking revealed that the estrogen receptor 1 and viral NS1 were potential targets at the late infection stage. The interactions could attenuate dengue productivity by interfering with viral translation and suppressing the viral proteins from trafficking to the cell surface.
Forthrightly monitoring ferroptosis induced by endoplasmic reticulum stresses through fluorescence lifetime imaging of microviscosity increases with a specific rotor
Liu, Chuanhao,Man, Huizi,Xiao, Yi,Xie, Lijuan,Zheng, Ying,Zhou, Lin
supporting information, (2022/01/08)
To test the hypothesis that the microviscosity changes of Endoplasmic Reticulum (ER) can be a useful indicator of ferroptosis promoted by ER Stresses (ERS), a new ER targeting viscosity rotor, L-Vis-1 was developed and applied in the quantitation of visco
