62351-50-2Relevant academic research and scientific papers
Novel β?hydroxy ketones: Synthesis, spectroscopic characterization, molecular docking, and anticancer activity studies
Guzel, Mustafa,Kanturk, Gokhan,Kucuk, Hatice Baspinar,Senturk, Ahmet Mesut,Yerlikaya, Serife,Yildiz, Tulay
, (2021/11/01)
In this study, a series of novel β?hydroxy ketone derivatives 3a-o were designed, synthesized, and evaluated for their anticancer activity. The structure of these compounds were characterized by IR, 1H and 13C NMR, mass spectrometry and elemental analysis methods. All the synthesized compounds were screened for anticancer activity against MCF-7 and U87 cells. Among them, compound 3l was appeared to be the most potent compound on both cancer cells; and IC50 dose was determined as 145 μM for MCF-7 cells and 6,6 μM for U87 cells. DNA ladder and Annexin V apoptotic marker tests were used and as a result, 3l caused the initiation of apoptosis on U87 cells. VDAC protein expression increased dramatically after U87 glioblastoma brain cancer cells were treated with compound 3l Additionally, the molecular modeling of these compounds was studied in FLT3 receptor, Estrogen receptor, and PARP2 receptor for the treatment of Acute Myeloid Leukemia (AML), breast cancer, and Glioblastoma (GBM) respectively. Their binding motifs and drug-like properties were investigated, and the results are highlighted in the discussion. Based on the results, compound 3l may have a potential drug candidate profile that can reverse the drug resistance profile.
Direct C-S bond formation: Via C-O bond activation of phenols in a crossover Pd/Cu dual-metal catalysis system
Khakyzadeh, Vahid,Rostami, Abed,Veisi, Hojat,Shirmardi Shaghasemi, Behzad,Reimhult, Erik,Luque, Rafael,Xia, Yuanzhi,Darvishi, Sima
, p. 4491 - 4497 (2019/05/17)
A dual-metal catalysis system including a newly prepared nanoparticle [SiO2@organic-linker(OL)@Pd(II)] and CuI was introduced with ultra-high catalytic activity (high turnover number (TON), up to 19000) to a one-pot and odorless synthesis of unsymmetrical aryl sulfides by crossover C-S bond formation. The reaction proceeds via C-O bond activation of phenols and direct C-S bond formation in the presence of S8 as an oddorless sulfur source and aryl boronic acids under mild conditions (room temperature). The catalyst could be recycled up to five times without an obvious change in its activity.
Synthesis of new thioxanthenes by organocatalytic intramolecular Friedel–Crafts reaction
Yildiz, Tülay
supporting information, p. 2177 - 2188 (2018/07/21)
An efficient organocatalytic route has been developed to synthesize novel substituted thioxanthenes (2a–2v) starting from diaryl thioether alcohols (1a–1v) using the intramolecular Friedel–Crafts reaction. The starting materials were obtained in two stage
Synthesis of diaryl sulfides via nickel ferrite-catalysed C─S bond formation in green media
Farzin, Shiva,Rahimi, Abdollah,Amiri, Kamran,Rostami, Abed,Rostami, Amin
, (2018/08/07)
NiFe2O4 magnetic nanoparticles (MNPs) were synthesized, characterized and applied as an air-stable, inexpensive and magnetically separable nanocatalyst for the synthesis of structurally diverse sulfides. Efficient methodologies were developed for the synthesis of unsymmetric diaryl sulfides via odourless and one-pot reactions of triphenyltin chloride/S8 or arylboronic acid/S8 as thiolating agents with aryl halides or nitroarenes as starting materials in the presence of base (K2CO3 or NaOH) and NiFe2O4 MNPs as a catalyst in water or poly (ethylene glycol) as solvent at 80–110?°C. Free from ligand and the unpleasant smell of thiols and with the use of magnetically reusable nanocatalyst, green solvents and commercially available and cheap sulfur source and starting materials, these methods are more eco-friendly and practical than available protocols for the synthesis of sulfides.
Metal-free oxidative coupling: Xanthone formation via direct annulation of 2-aryloxybenzaldehyde using tetrabutylammonium bromide as a promoter in aqueous medium
Rao, Honghua,Ma, Xinyi,Liu, Qianzi,Li, Zhongfeng,Cao, Shengli,Li, Chao-Jun
supporting information, p. 2191 - 2196 (2013/10/01)
A metal-free intramolecular annulation of 2-aryloxybenzaldehydes to xanthones is disclosed, which proceeds through the direct oxidative coupling of an aldehyde C-H bond and aromatic C-H bonds using tetrabutylammonium bromide (TBAB) as a promoter in aqueous medium. This strategy works smoothly in the presence of both electron-donating and electron-withdrawing groups, and displays good tolerance towards catalytically reactive substituents, thus promising further functionalizations of xanthone products.
Copper-catalyzed activation of disulfides as a key step in the synthesis of benzothiazole moieties
Hyvl, Jakub,Srogl, Jiri
supporting information; experimental part, p. 2849 - 2851 (2010/07/18)
A convenient synthesis of substituted benzothiazoles has been accomplished by way of a copper catalyzed reaction of aromatic disulfide amines and aldehydes. The process, which involves copper catalyzed activation of disulfide functionality, proceeds in a
Novel amides that activate soluble guanylate cyclase
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, (2008/06/13)
Compounds of formula (I) are useful for increasing cGMP levels in a mammal.
Novel amides that activate soluble guanylate cyclase
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Page 12, (2010/02/08)
Compounds of formula (I) are useful for increasing cGMP levels in a mammal.
A concise synthesis of ortho-substituted aryl-acrylamides - Potent activators of soluble guanylyl cyclase
Zhang, Henry Q.,Xia, Zhiren,Kolasa, Teodozyj,Dinges, Jurgen
, p. 8661 - 8663 (2007/10/03)
Horner-Emmons reaction of phosphonate amides with aldehydes leads to generation of o-substituted aryl-acrylamides. These compounds have been shown to be useful to quickly establish structure-activity relationships (SAR) for soluble guanylyl cyclase (sGC)
Syntheses of o/p-arylthiobenzaldehydes and o/p-methylsulphonylbenzaldehydes
Sivasubramanian, S,Ravichandran, K
, p. 1148 - 1149 (2007/10/02)
A general synthesis of o/p-arylthiobenzaldehydes starting from the corresponding chlorobenzaldehydes and an efficient conversion of o/p-methylbenzenethiols to o/p-methylsulphonylbenzaldehydes are described.
