36874-95-0Relevant academic research and scientific papers
DIAMINE OXIDASE FROM LENS ESCULENTA SEEDLINGS: PURIFICATION AND PROPERTIES
Floris, Giovanni,Giartosio, Anna,Rinaldi, Augusto
, p. 1871 - 1874 (1983)
A diamine oxidase (DAO) (EC 1.4.3.6) has been purified to homogeneity from lentil seedlings.The purified protein has a MW of 154000 and is composed of two apparently identical subunits.It contains two Cu(2+) atoms and one carbonyl-like group per mol.The purified enzyme is pink-red in concentrated solution and shows a broad, well-defined, absorption band in the visible region centered at 498 nm.The ESR spectrum is typical of Cu(2+) in a tetragonal symmetry.The enzyme oxidizes only aliphatic diamines and spermidine with formation of the corresponding aldehydes, hydrogen peroxide and ammonia.Putrescine and cadaverine are oxidized most rapidly and the oxidation rate decreases when longer diamines are tested. - Key Word Index - Lens esculenta; Leguminosae; lentil seedlings; copper protein; diamine oxidase.
Development of a water-soluble 3-formylBODIPY dye for fluorogenic sensing and cell imaging of sulfur dioxide derivatives
I??k, Murat,Simsek Turan, Ilke,Dartar, Suay
supporting information, p. 1421 - 1425 (2019/04/30)
A new water-soluble, highly fluorogenic 3-formylBODIPY dye that enables the sensing of SO2 derivatives in aqueous buffers and cancer cells is reported. The quaternary ammonium group appended through the meso-position of the BODIPY dye ensures water solubility. The probe exhibits high specificity for cytosolic (bi)sulfites and fluoresces brightly in human lung adenocarcinoma cells (A549).
Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers
Wang, Caolin,Xu, Shan,Peng, Liang,Zhang, Bingliang,Zhang, Hong,Hu, Yingying,Zheng, Pengwu,Zhu, Wufu
, p. 204 - 218 (2019/01/03)
A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT with the IC50 value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFRL858R/T790M (0.1 μM). Excitingly, the most potent compound 14 showed excellent enzyme inhibitory activity with 6.3 nM and 8.4 nM for both EGFRWT and EGFRT790M/L858R. The result of AO single staining and Annexin V/PI staining showed that the compound 14 and 44 could induce remarkable apoptosis of A549 cells. The compound 14 arrested the cell cycle at the S phase and compound 44 arrested the cell cycle at the G0 phase in A549 cells. These preliminary results demonstrate that compound 14 and 44 may be promising lead compound-targeting EGFR.
Fluorescent probe for continuously recognizing palladium ions and CO and application
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Paragraph 0020, (2017/06/14)
The invention provides a fluorescent probe for continuously recognizing palladium ions and CO. The fluorescent probe is 1-4-(1 hydrogen-phenanthrenequinone [9,10-d] imidazole-2-ethyl) phenyl N,N-dimethyl methylamine, which is abbreviated as PIPD. The invention further discloses application of the fluorescent probe in specifically recognizing divalent palladium ions in a water phase. By adopting the palladium ion fluorescent probe provided by the invention, the palladium ions can be selectively detected in the water phase, fluorescence quenching can be implemented, and the fluorescence can be quenched again if a biological CO reagent is used. Due to the AIE characteristic, the fluorescent probe has outstanding advantages in detecting living bodies, and has potential application values in the field of laser excited fluorescence biomarkers.
Water-soluble red-emitting distyryl-borondipyrromethene (BODIPY) dyes for biolabeling
Niu, Song-Lin,Massif, Cedrik,Ulrich, Gilles,Renard, Pierre-Yves,Romieu, Anthony,Ziessel, Raymond
, p. 7229 - 7242 (2012/07/03)
A series of water-soluble red-emitting distyryl-borondipyrromethene (BODIPY) dyes were designed and synthesized by using three complementary approaches aimed at introducing water-solubilizing groups on opposite faces of the fluorescent core to reduce or c
METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)
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, (2011/11/01)
Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.
DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 55-56, (2010/03/02)
A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation and structure-activity relationships. Part 2
Horiuchi, Takao,Nagata, Motoko,Kitagawa, Mayumi,Akahane, Kouichi,Uoto, Kouichi
experimental part, p. 7850 - 7860 (2010/04/02)
The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl group
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives
Sheng, Rong,Xu, Yu,Hu, Chunqi,Zhang, Jing,Lin, Xiao,Li, Jingya,Yang, Bo,He, Qiaojun,Hu, Yongzhou
experimental part, p. 7 - 17 (2009/04/06)
A new series of indanone and aurone derivatives have been synthesized and tested for in vitro AChE inhibitory activity by modified Ellman method. Most of them exhibit AChE inhibitory activities superior to rivastigmine. Further, the most potent compound 1g was selected to evaluate the effect on the acquisition and memory impairment by mice step-down passive avoidance test.
HYDRAZONE DERIVATIVE
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Page/Page column 39, (2010/11/08)
A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
