128958-85-0Relevant 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.
Formation and Disproportionation of Xanthenols to Xanthenes and Xanthones and Their Use in Synthesis
Shi, Zeyu,Chen, Si,Xiao, Qiong,Yin, Dali
, p. 3334 - 3343 (2021/02/05)
A facile and versatile strategy employing TiCl4-mediated cyclization followed by a Cannizzaro reaction has been developed for the synthesis of various xanthene derivatives. The reaction proceeded smoothly to afford both xanthenes/xanthones or their sulfur derivatives and tolerated a wide range of electronically diverse substrates. Using this methodology, pranoprofen was synthesized in three steps in 59% overall yield from commercially available starting materials.
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
New CRTH2 Antagonists
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Page/Page column 25, (2012/12/13)
The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
Palladium-catalyzed carbon-sulfur cross-coupling reactions with indium tri(organothiolate) and its application to sequential one-pot processes
Lee, Jae-Young,Phil, Ho Lee
supporting information; experimental part, p. 7413 - 7416 (2009/05/07)
(Chemical Equation Presented) It was found that indium tri(organothiolate) is an effective nucleophilic coupling partner in Pd-catalyzed C-S cross-coupling reactions to produce the functionalized sulfides in excellent yields with high atom efficiency and
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.
POTENTIAL ANTIDEPRESSANTS: 1-(2-(METHOXY- AND HYDROXY-PHENYLTHIO)PHENYL)-2-PROPYLAMINES
Urban, Jiri,Sedivy, Zdenek,Holubek, Jiri,Svatek, Emil,Ryska, Miroslav,et al.
, p. 1077 - 1098 (2007/10/02)
2-(Methoxyphenylthio)benzaldehydes Xa-Xd were reacted with nitroethane in boiling acetic acid to give the corresponding 1-aryl-2-nitropropenes XIIa-XIId: benzonitriles XIIIa and XIIIc and benzaldoximes XXIc and XXId were isolated as by-products.Chromatogr
