72785-29-6Relevant academic research and scientific papers
4,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin
Wang, Zhiwei,Qi, Huan,Shen, Qirong,Lu, Guodong,Li, Mingyang,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 520 - 529 (2016)
A new series of 4,5-diaryl-3H-1,2-dithiole-3-thiones and related compounds were designed and synthesised as combretastatin A-4/oltipraz hybrids. We evaluated the antiproliferative activities, inhibition of tubulin polymerization, and cell-cycle effects of
TRICYCLIC PIPERIDINE COMPOUNDS
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Page/Page column 77, (2016/11/21)
The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, (R4)n and ring (A) are as described in the description, to their preparation, to pharmaceutically acc
Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid
Lee, Yun Suk,Kim, Hye Yun,Kim, Youngsoo,Seo, Jae Hong,Roh, Eun Joo,Han, Hogyu,Shin, Kye Jung
experimental part, p. 4921 - 4935 (2012/10/08)
Aggregated β-amyloid (Aβ) plays crucial roles in Alzheimer's disease (AD) pathogenesis, therefore blockade of Aβ aggregation is considered as a potential therapeutic target. We designed and synthesized small molecules to reduce Aβ-induced cytotoxicity by inhibiting Aβ aggregation. The small molecules were screened via ThT, MTT, and cell-based cytotoxicity assay (Aβ burden assay). Selected compounds 1c, 1d, 1e, and 1f were then investigated by evaluating their effects on cognitive impairment of acute AD mice model. Learning and memory dysfunction by injection of Aβ(1-42) was recovered by administration of these molecules. Especially, 1d showed the best recovery activity in Y-maze task, object recognition task, and passive avoidance task with dose dependent manner. These results suggest that 1d has high potential as a therapeutic agent for AD.
Novel diarylheptanoids as inhibitors of TNF-α production
Dhuru, Sameer,Bhedi, Dilip,Gophane, Dnyaneshwar,Hirbhagat, Kiran,Nadar, Vijaya,More, Dattatray,Parikh, Sapna,Dalal, Roda,Fonseca, Lyle C.,Kharas, Firuza,Vadnal, Prashant Y.,Vishwakarma, Ram A.,Sivaramakrishnan
supporting information; experimental part, p. 3784 - 3787 (2011/07/31)
Synthesis and anti-inflammatory activity of novel diarylheptanoids [5-hydroxy-1-phenyl-7-(pyridin-3-yl)-heptan-3-ones and 1-phenyl-7-(pyridin-3-yl) hept-4-en-3-ones] as inhibitors of tumor necrosis factor-α (TNF-α) production is described in the present article. The key reactions involve the formation of a β-hydroxyketone by the reaction of substituted 4-phenyl butan-2-ones with pyridine-3-carboxaldehyde in presence of LDA and the subsequent dehydration of the same to obtain the α,β-unsaturated ketones. Compounds 4i, 5b, 5d, and 5g significantly inhibit lipopolysaccharide (LPS)-induced TNF-α production from human peripheral blood mononuclear cells in a dose-dependent manner. Of note, the in vitro TNF-α inhibition potential of 5b and 5d is comparable to that of curcumin (a naturally occurring diarylheptanoid). Most importantly, oral administration of 4i, 5b, 5d, and 5g (each at 100 mg/kg) but not curcumin (at 100 mg/kg) significantly inhibits LPS-induced TNF-α production in BALB/c mice. Collectively, our findings indicate that these compounds may have potential therapeutic implications for TNF-α-mediated auto-immune/inflammatory disorders.
Synthesis of 5-substituted benzyl-2,4-diamino pyrimidine derivatives as c-Fms kinase inhibitors
Xu, Li Bao,Sun, Wei,Liu, Hong Ying,Wang, Li Li,Xiao, Jun Hai,Yang, Xiao Hong,Li, Song
scheme or table, p. 1318 - 1321 (2011/10/09)
A serials of novel 5-substituted benzyl-2,4-diamino pyrimidine derivatives have been synthesized and evaluated as inhibitors of c-Fms kinase by the standard MTT method. The results showed that compound 15,5-[3-methoxy-4-(pyridine-3-yl)benzyl]-2,4-diamino pyrimidine, had an IC50 of 1.45μmol/L in inhibiting the proliferation of M-CSF-dependent myeloid leukemia cells in mice (NFS-60), which was similar with GW2580, a selective inhibitor of c-Fms kinase.
Efficient preparation and processing of the 4-methoxybenzyl (PMB) group for phenolic protection using ultrasound
Luzzio, Frederick A.,Chen, Juan
, p. 5621 - 5624 (2008/12/21)
(Chemical Equation Presented) Power ultrasound efficiently facilitates the rapid preparation and reaction of 4-methoxybenzyl chloride (PMB-Cl) 1 in providing protected phenolic ether intermediates for organic synthesis. Using two-phase systems in both the ultrasound-promoted preparation and reactions of PMB-Cl, typical runs produce PMB-protected products within 15 min. When compared with nonsonicated control reactions, the results demonstrate clear advantage in terms of efficiency when the protocol is applied to the mild and selective protection of various multisubstituted phenols including sensitive phenolic aldehydes.
Regioselective protection of the 4-hydroxyl of 3,4-dihydroxy-benzaldehyde
Plourde, Guy L.,Spaetzel, Randy R.
, p. 697 - 705 (2007/10/03)
The regioselective protection of the 4-hydroxyl group of 3,4-dihydroxy-benzaldehyde was accomplished with seven different protecting groups (benzyl, p-methoxybenzyl, o-nitrobenzyl, 2,6-dichlorobenzyl, 3,4-dichlorobenzyl, vinyl and propargyl) in yields ranging between 67-75percent.
SYNTHESIS OF GALANTHAMINE AND RELATED ALKALOIDS - NEW APPROARCHES. I.
Vlahov, Radoslav,Krikorian, Dikran,Spassov, Grigor,Chinova, Maja,Vlahov, Ioncho,et al.
, p. 3329 - 3346 (2007/10/02)
Modifications of protecting groups and of the oxidative coupling conditions led to pure crystalline intermediates in the synthesis of galanthamine derivatives and gave dienone A in better yields than reported before.The E-configuration of amide 3' in crystalline state has been determined by X-ray diffraction.Streptomyces affinis 6737 reduces A to the optically active (-)-epigalanthamine derivative C, whose absolute configuration was determined by Bijvoet's method.Nematospora corylii CBS 2608 reduces to racemic B.With Ashbya gossypii IFO 1355 a mixture of racemic B and of optically active C is obtained.Some other microbial transformations are described.
