34859-82-0Relevant academic research and scientific papers
Structural optimization and structure–activity relationship of 4-thiazolidinone derivatives as novel inhibitors of human dihydroorotate dehydrogenase
Zeng, Fanxun,Quan, Lina,Yang, Guantian,Qi, Tiantian,Zhang, Letian,Li, Shiliang,Li, Honglin,Zhu, Lili,Xu, Xiaoyong
, (2019/08/07)
Human dihydroorotate dehydrogenase (hDHODH), one of the attractive targets for the development of immunosuppressive drugs, is also a potential target of anticancer drugs and anti-leukemic drugs. The development of promising hDHODH inhibitors is in high demand. Based on the unique binding mode of our previous reported 4-thiazolidinone derivatives, via molecular docking method, three new series 4-thiazolidinone derivatives were designed and synthesized as hDHODH inhibitors. The preliminary structure–activity relationship was investigated. Compound 9 of biphenyl series and compound 37 of amide series displayed IC50 values of 1.32 μM and 1.45 μM, respectively. This research will provide valuable reference for the research of new structures of hDHODH inhibitors.
Inhibitors of notch signalling pathway and use thereof in treatment of cancers
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Page/Page column 39; 41, (2016/04/26)
The present invention relates to use of inhibitors of Notch signalling pathway selected from the group consisting of 6-(4-Tert-Butylphenoxy)Pyridin-3-Amine (I3), its derivatives, in treating and/or preventing cancers.
CsF/clinoptilolite: An efficient solid base in SNAr and copper-catalyzed Ullmann reactions
Keipour, Hoda,Hosseini, Abolfazl,Afsari, Amir,Oladee, Razieh,Khalilzadeh, Mohammad A.,Ollevier, Thierry
, p. 95 - 104 (2016/01/16)
CsF/clinoptilolite was found to be an efficient solid base catalyst for both SNAr and Ullmann ether reactions. A general and efficient one-step procedure was developed for the synthesis of biaryl ethers via direct coupling of electron-deficient aryl halides to phenols using CsF/clinoptilolite. The protocol was also applied to electron-rich aryl halides by addition of a catalytic amount of copper oxide nanoparticles. Both SNAr and Ullmann reactions were rapid and provided good to excellent yields.
Maghemite-Copper Nanocomposites: Applications for Ligand-Free Cross-Coupling (C-O, C-S, and C-N) Reactions
Sharma, Rakesh K.,Gaur, Rashmi,Yadav, Manavi,Rathi, Anuj K.,Pechousek, Jiri,Petr, Martin,Zboril, Radek,Gawande, Manoj B.
, p. 3495 - 3502 (2015/11/10)
A magnetically retrievable, efficient, and benign maghemite-Cu nanocatalyst was synthesized from inexpensive precursors and applied for C-O, C-N, and C-S bond-formation reactions. The obtained maghemite-Cu nanocatalyst was characterized by various techniques such as XRD, X-ray photoelectron spectroscopy, field-emission gun SEM with energy-dispersive spectroscopy, atomic absorption spectroscopy, TEM, high-angle annular dark-field scanning transmission electron microscopy, FTIR spectroscopy, and M?ssbauer spectroscopy. Excellent catalytic activity, ease of recovery, and reusability without a significant loss of yield make the present protocol highly sustainable to deal with industrial and environmental concerns. Magnetic attraction: A magnetically retrievable, efficient, and benign maghemite-Cu nanocatalyst is synthesized from inexpensive precursors and applied for C-O, C-N, and C-S bond-formation reactions. Excellent catalytic activity, ease of recovery, and reusability without significant loss of yield make the present protocol highly sustainable to deal with industrial and environmental concerns.
Palladium nanoparticles supported on natural nanozeolite clinoptilolite as a catalyst for ligand and copper-free C-C and C-O cross coupling reactions in aqueous medium
Baghbanian, Seyed Meysam,Yadollahy, Horieh,Tajbakhsh, Mahmood,Farhang, Maryam,Biparva, Pourya
, p. 62532 - 62543 (2015/02/19)
In this article, Pd0-nanoparticles supported on natural nanozeolite clinoptilolite (CP) were successfully synthesized, and the catalytic activity of the nanocatalyst was investigated in C-C and C-O coupling reactions, namely the Sonogashira and Ullmann condensation reactions in an aqueous medium. The nanocatalyst was characterized by various techniques such as powder-XRD, BET, SEM, TEM, HRTEM, TEM-EDS, ICP-OES and XPS. From an electron microscopy (SEM) study it can be inferred that the particles are mostly spherical or of ellipsoidal shape and have diameters ranging from 25 to 80 nm. A HRTEM study reveals that Pd0-nanoparticles supported on nanozeolite CP have an average diameter of ~10 nm. The supported palladium nanoparticles showed excellent catalytic activity in the synthesis of aryl alkynes and diaryl ethers in high yields. In addition, the nanocatalyst could be recycled and reused several times without significant loss of catalytic activity.
Magnetically retrievable nano crystalline nickel ferrite- catalyzed aerobic, ligand-free C-N, C-O and C-C cross-coupling reactions for the synthesis of a diversified library of heterocyclic molecules
Paul, Sanjay,Pradhan, Koyel,Ghosh, Sirshendu,De,Das, Asish R.
, p. 1301 - 1316 (2014/05/06)
A new nickel ferrite nano-crystal-catalyzed, ligand-free strategy for the construction of C-N, C-O, and C-C bonds is presented, in which easily available nitrogen and oxygen nucleophiles, aryl/heteroaryl halides and arylboronic acids are used for the cross-coupling reactions. The reactions can be performed at low catalyst loadings with excellent functional group tolerance and chemoselectivity. A variety of functional groups are compatible with the reaction conditions, including nitro, methoxy, as well as acid- and base-sensitive heteroaromatic groups. This unprecedented chemistry nicely complements classical methods for the N-arylation of amines/heteroamines, the O-arylation of phenols/hydroxycoumarins and biaryl/heteroaryl synthesis. The low cost, easy to handle nature and the simplicity of this catalytic system render the method competitive with comparable copper- and palladium-based protocols which require the presence of sophisticated ligands. Nickel ferrite magnetic nanoparticles were prepared by a simple hydrothermal method and characterized by using XRD, TEM image, energy dispersive X-ray analysis, XPS and FT-IR. The easy recovery of the catalyst and high yield of the products make the protocol attractive, sustainable and economic. The catalyst was reused for five cycles with almost unaltered catalytic activity.
Facile preparation of unsymmetrical diaryl ethers from unsymmetrical diaryliodonium tosylates and phenols with high regioselectivity
Kakinuma, Yohji,Moriyama, Katsuhiko,Togo, Hideo
, p. 183 - 188 (2013/02/23)
Unsymmetrical diaryl ethers were efficiently obtained in good yields by the reactions of aryl(4-methoxyphenyl)iodonium tosylates with phenols, and aryl(2,4-dimethoxyphenyl)iodonium tosylates with phenols, in the presence of potassium carbonate in acetonitrile, respectively. The latter iodonium tosylates provided the corresponding unsymmetrical diaryl ethers in good yields with high regioselectivities, together with the quantitative formation of 1-iodo-2,4-dimethoxybenzene. Georg Thieme Verlag Stuttgart New York.
INHIBITORS OF NOTCH SIGNALLING PATHWAY AND USE THEREOF IN TREATMENT OF CANCERS
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Page/Page column 56, (2013/07/05)
The present invention relates to use of inhibitors of Notch signalling pathway selected from the group consisting of 6-(4-Tert-Butylphenoxy)Pyridin-3-Amine (I3), its derivatives, in treating and/or preventing cancers.
Palladium supported on zinc ferrite: An efficient catalyst for ligand free C-C and C-O cross coupling reactions
Singh, Abhilash S.,Shendage, Suresh S.,Nagarkar, Jayashree M.
, p. 6319 - 6323 (2013/11/06)
An efficient superparamagnetic Pd-ZnFe2O4 solid catalyst has been synthesized by loading Pd(0) species on zinc ferrite nanoparticles. Sonogashira cross couplings between terminal alkynes and aryl halides were achieved in the absence of any Cu co-catalyst. A Heck-Matsuda coupling reaction of structurally different aryldiazonium tetrafluoroborate substrates was preceded at 40 C in water. Cyanation of aryl halides was successfully done using K4[Fe(CN)6] as the cyanide source over Pd-ZnFe2O4. The catalyst was also employed for Ullmann type cross coupling reactions. Excellent yield of the products, reusability, and uncomplicated work-up make this catalyst efficient for C-C and C-O coupling reactions. Good yield of products, easy separation, and negligible leaching of Pd from the catalyst surface confirm the true heterogeneity in these catalytic reactions.
Potassium fluoride supported on natural nanoporous zeolite: A new solid base for the synthesis of diaryl ethers
Khalilzadeh, Mohammad A.,Hosseini, Abolfazl,Pilevar, Afsaneh
experimental part, p. 1587 - 1592 (2011/04/22)
An efficient and inexpensive synthesis of diaryl ethers has been developed. The process involves the nucleophilic aromatic substitution of electron-deficient aryl halides and phenols and is mediated by potassium fluoride/Clinoptilolite (KF/CP) in dimethyl sulfoxide (DMSO). The approach affords good to excellent yields of the arylated products without the need for additional cation capture. The solid base is also efficient in the Ullmann ether synthesis. A new, inexpensive solid base for the synthesis of diaryl ethers has been developed. Clinoptilolite, a natural zeolite with a high tendency for cation capture, combined with potassium fluoride, provides an efficientsolid base for the deprotonation of phenols in nucleophilic reactions. The same solid base acts as a reliable base for the copper-catalyzed synthesis of diaryl ethers. Copyright
