307973-30-4Relevant academic research and scientific papers
Synthesis of unsymmetrical monocarbonyl curcumin analogues with potent inhibition on prostaglandin E2 production in LPS-induced murine and human macrophages cell lines
Mohd Aluwi, Mohd Fadhlizil Fasihi,Rullah, Kamal,Yamin, Bohari M.,Leong, Sze Wei,Abdul Bahari, Mohd Nazri,Lim, Sock Jin,Mohd Faudzi, Siti Munirah,Jalil, Juriyati,Abas, Faridah,Mohd Fauzi, Norsyahida,Ismail, Nor Hadiani,Jantan, Ibrahim,Lam, Kok Wai
, p. 2531 - 2538 (2016/07/07)
The syntheses and bioactivities of symmetrical curcumin and its analogues have been the subject of interest by many medicinal chemists and pharmacologists over the years. To improve our understanding, we have synthesized a series of unsymmetrical monocarbonyl curcumin analogues and evaluated their effects on prostaglandin E2 production in lipopolysaccharide-induced RAW264.7 and U937 cells. Initially, compounds 8b and 8c exhibited strong inhibition on the production of PGE2 in both LPS-stimulated RAW264.7 (8b, IC50 = 12.01 M and 8c, IC50 = 4.86 μM) and U937 (8b, IC50 = 3.44 μM and 8c, IC50 = 1.65 μM) cells. Placing vanillin at position Ar2 further improved the potency when both compounds 15a and 15b significantly lowered the PGE2 secretion level (RAW264.7: 15a, IC50 = 0.78 μM and 15b, IC50 = 1.9 μM while U937: 15a, IC50 = 0.95 μM and 15b, IC50 = 0.92 μM). Further experiment showed that compounds 8b, 8c, 15a and 15b did not target the activity of downstream inflammatory COX-2 mediator. Finally, docking simulation on protein targets COX-2, IKK-β, ERK, JNK2, p38α and p38β were performed using the conformation of 15a determined by single-crystal XRD.
New compounds having skin whitening activity and medical use thereof
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Paragraph 0039-0046, (2021/11/10)
The present invention relates to novel compounds having skin whitening activity and a medical use thereof, wherein the novel compounds are represented by chemical formula 1. The compounds according to the present invention have skin whitening activity that inhibits tyrosinase, thereby being used as a pharmaceutical composition, a cosmetic composition, or a functional health food for skin whitening.
Fe3O4 nanoparticles as an efficient and magnetically recoverable catalyst for the synthesis of α β-unsaturated heterocyclic and cyclic ketones under solvent-free conditions
Alishiri, Tooba,Oskooei, Hossein A.,Heravi, Majid M.
, p. 3357 - 3362 (2013/10/01)
An efficient and green procedure has been developed for the synthesis of monoarylidenes of cyclic and heterocyclic ketones. The reaction was carried out under solvent-free conditions in the presence of a catalytic amount of nanosized magnetite (Fe3O4). The catalyst was easily removed by using an external magnet. The structures of the products were deduced from their 1H NMR, 13C NMR, and infrared spectroscopy and mass spectrometry. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]
Sequential cytotoxicity: A theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds
Dimmock,Kandepu,Nazarali,Motaganahalli,Kowalchuk,Pugazhenthi,Prisciak,Quail,Allen,LeClerc,Santos,De Clercq,Balzarini
, p. 3933 - 3940 (2007/10/03)
Five series of novel compounds were synthesized in order to evaluate the theory of sequential cytotoxicity which seeks to exploit the view that various cancer cells are particularly susceptible to successive attacks by cytotoxic agents. The compounds prep
Cytotoxic 2,6-bis(arylidene)cyclohexanones and related compounds
Dimmock, Jonathan R.,Kumar, Praveen,Nazarali, Adil J.,Motaganahalli, Narasimhan L.,Kowalchuk, Travis P.,Beazely, Michael A.,Wilson Quail,Oloo, Eliud O.,Allen, Theresa M.,Szydlowski, Jennifer,DeClercq, Erik,Balzarini, Jan
, p. 967 - 977 (2007/10/03)
A number of 2-arylidenecyclohexanones 1, 2,6-bis(arylidene)cyclohexanones 2 and related Mannich bases 3-5 were prepared. Various torsion angles as well as atomic charges on olefinic carbon atoms were determined by molecular modelling on all compounds. These molecules showed cytotoxicity towards murine P388 and L1210 cells as well as to human Molt 4/C8 and CEM T-lymphocytes. The average cytotoxicity of the dienones 2 was more than three times greater than was found with the monoarylidene analogues 1, and, in general, were slightly more cytotoxic than the Mannich bases 3-5. A number of the compounds displayed potency towards a panel of human tumour cell lines and most of the representative compounds in series 2-5 were selectively toxic to colon cancers and leukaemic cells. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
Towards peptide isostere libraries: Aqueous aldol reactions on hydrophilic solid supports
Graven, Anette,Grotli, Morten,Meldal, Morten
, p. 955 - 962 (2007/10/03)
Polar polyoxyethylene-polyoxypropylene (POEPOP) resin was derivatised with a 4-hydroxymethyl phenoxy linker and used as a solid support for lanthanide triflate catalysed Mukaiyama type solid phase aldol reactions. The conditions were optimised using resin bound 4-alkoxybenzaldehyde and it was shown that use of an aqueous solvent was crucial. Also, the reactions were performed with an N-terminal peptide aldehyde substrate in very high yields. POEPOP resins prepared with different monomer chain lengths and commercially available PEG-grafted NovaSyn TG resin were compared in the reactions.
