613-94-5Relevant articles and documents
Highly selective colorimetric fluorescent sensor for Pb2+
Goswami, Shyamaprosad,Chakrabarty, Rinku
, p. 3791 - 3795 (2010)
Phenanthroline-based colorimetric sensors 1 and 2 have been designed, synthesized, and compared with phenanthrene-based receptor 3 for sensing of Pb2+ by color change. Receptor 1 imparts color change (from yellow to red) selectively with Pb2+ in acetonitrile/water (9:1) as well as in methanol/water (9:1) when in the presence of other metal ions studied (Li +, Na+, K+, Ca2+, Mg2+, Ba2+, Fe3+, Co2+, Ni2+, Cu 2+, Zn2+, Cd2+, Hg2+, and Mn 2+ as their Perchlorate salts). Receptor 1 also shows fluorescence enhancement upon addition of lead Perchlorate in acetonitrile/water (9:1) solvent possibly due to the chelation enhanced fluorescence (CHEF) effect. However, the binding behavior of 2 with Pb2+ is found to be less effective compared to that of receptor 1.
Synthesis, characterization, thermal degradation and urease inhibitory studies of the new hydrazide based Schiff base ligand 2-(2-hydroxyphenyl)-3-{[(E)-(2-hydroxyphenyl)methylidene]amino}-2,3-dihydroquinazolin-4(1H)-one
Ikram, Muhammad,Rehman, Sadia,Subhan, Fazle,Akhtar, Muhammad Nadeem,Sinnokrot, Mutasem Omar
, p. 308 - 319 (2017)
The novel Schiff base ligand 2-(2-hydroxyphenyl)-3-{[(E)-(2-hydroxyphenyl)methylidene]amino}-2,3-dihydroquinazolin-4(1H)-one (H-HHAQ) derived from 2-aminobenzhydrazide was synthesized and characterized by elemental analyses, ES+-MS, 1/sup
A new strategy for fluorometric detection of ascorbic acid based on hydrolysis and redox reaction
Zhao, Yirong,Li, Yinhui,Wang, Yijun,Zheng, Jing,Yang, Ronghua
, p. 35112 - 35115 (2014)
In this study, a near-infrared, indole-cyanine probe, i.e. Cy5-HD, was designed for the detection of ascorbic acid for the first time. The probe has a hydrazone moiety that can be hydrolyzed by Cu2+ to induce the fluorescence quenching of Cy5-H
Protein-Metal-Ion Interactions Studied by Mass Spectrometry-Based Footprinting with Isotope-Encoded Benzhydrazide
Guo, Chunyang,Cheng, Ming,Gross, Michael L.
, p. 1416 - 1423 (2019)
Metal ions, usually bound by various amino-acid side chains in proteins, play multiple roles in protein folding, conformational change, cellular communication, and catalysis. Ca(II) and Mg(II), abundant among biologically relevant cations, execute their c
Exploration of synthesis, structural aspects, DFT studies and bio-efficacy of some new DHA-benzohydrazide based copper(II) complexes
Richa,Kumar, Sunil,Sindhu, Jayant,Choudhary, Poonam,Jaglan, Sundeep,Zangrando, Ennio,Kumar, Rakesh,Sahoo, Subash C.,Kumar, Vinod,Mehta, Surinder K.,Kataria, Ramesh
, (2021)
A copper (II) complex with ligand obtained by the dehydrative condensation of 3-acetyl-6-methyl-2H-pyran-2,4(3H)?dione (DHA) and benzohydrazide has been synthesized (4). This species was additionally coordinated by various solvent molecules, namely ethano
Design, synthesis and pharmacological evaluation of tricyclic derivatives as selective RXFP4 agonists
Lin, Lin,Lin, Guangyao,Zhou, Qingtong,Bathgate, Ross A.D.,Gong, Grace Qun,Yang, Dehua,Liu, Qing,Wang, Ming-Wei
supporting information, (2021/03/16)
Relaxin family peptide receptors (RXFPs) are the potential therapeutic targets for neurological, cardiovascular, and metabolic indications. Among them, RXFP3 and RXFP4 (formerly known as GPR100 or GPCR142) are homologous class A G protein-coupled receptors with short N-terminal domain. Ligands of RXFP3 or RXFP4 are only limited to endogenous peptides and their analogues, and no natural product or synthetic agonists have been reported to date except for a scaffold of indole-containing derivatives as dual agonists of RXFP3 and RXFP4. In this study, a new scaffold of tricyclic derivatives represented by compound 7a was disclosed as a selective RXFP4 agonist after a high-throughput screening campaign against a diverse library of 52,000 synthetic and natural compounds. Two rounds of structural modification around this scaffold were performed focusing on three parts: 2-chlorophenyl group, 4-hydroxylphenyl group and its skeleton including cyclohexane-1,3-dione and 1,2,4-triazole group. Compound 14b with a new skeleton of 7,9-dihydro-4H-thiopyrano[3,4-d][1,2,4]triazolo[1,5-a]pyrimidin-8(5H)-one was thus obtained. The enantiomers of 7a and 14b were also resolved with their 9-(S)-conformer favoring RXFP4 agonism. Compared with 7a, compound 9-(S)-14b exhibited 2.3-fold higher efficacy and better selectivity for RXFP4 (selective ratio of RXFP4 vs. RXFP3 for 9-(S)-14b and 7a were 26.9 and 13.9, respectively).
Design, synthesis, and anti-proliferative evaluation of new quinazolin-4(3H)-ones as potential VEGFR-2 inhibitors
El-Adl, Khaled,El-Helby, Abdel-Ghany A.,Ayyad, Rezk R.,Mahdy, Hazem A.,Khalifa, Mohamed M.,Elnagar, Hamdy A.,Mehany, Ahmed B.M.,Metwaly, Ahmed M.,Elhendawy, Mostafa A.,Radwan, Mohamed M.,ElSohly, Mahmoud A.,Eissa, Ibrahim H.
, (2020/11/24)
Inhibiting VEGFR-2 has been set up as a therapeutic strategy for treatment of cancer. Thus, nineteen new quinazoline-4(3H)-one derivatives were designed and synthesized. Preliminary cytotoxicity studies of the synthesized compounds were evaluated against three human cancer cell lines (HepG-2, MCF-7 and HCT-116) using MTT assay method. Doxorubicin and sorafenib were used as positive controls. Five compounds were found to have promising cytotoxic activities against all cell lines. Compound 16f, containing a 2-chloro-5-nitrophenyl group, has emerged as the most active member. It was approximately 4.39-, 5.73- and 1.96-fold more active than doxorubicin and 3.88-, 5.59- and 1.84-fold more active than sorafenib against HepG2, HCT-116 and MCF-7 cells, respectively. The most active cytotoxic agents were further evaluated in vitro for their VEGFR-2 inhibitory activities. The results of in vitro VEGFR-2 inhibition were consistent with that of the cytotoxicity data. Molecular docking of these compounds into the kinase domain, moreover, supported the results.