3558-83-6Relevant academic research and scientific papers
Synthesis and structure-activity relationship for new series of 4-phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase
Kubo, Kazuo,Ohyama, Shin-Ichi,Shimizu, Toshiyuki,Takami, Atsuya,Murooka, Hideko,Nishitoba, Tsuyoshi,Kato, Shinichiro,Yagi, Mikio,Kobayashi, Yoshiko,Iinuma, Noriko,Isoe, Toshiyuki,Nakamura, Kazuhide,Iijima, Hiroshi,Osawa, Tatsushi,Izawa, Toshio
, p. 5117 - 5133 (2007/10/03)
We discovered a new series of 4-phenoxyquinoline derivatives as potent and selective inhibitors of the platelet-derived growth factor receptor (PDGFr) tyrosine kinase. We researched the highly potent and selective inhibitors on the basis of both PDGFr and epidermal growth factor receptor (EGFr) inhibitory activity. First, we found a compound, Ki6783 (1), which inhibited PDGFr autophosphorylation at 0.13 μM, but it did not inhibit EGFr autophosphorylation at 100 μM. After extensive explorations, we found the two desired compounds, Ki6896 (2) and Ki6945 (3), which are substituted by benzoyl and benzamide at the 4-position of the phenoxy group on 4-phenoxyquinoline, respectively. These inhibitory activities were 0.31 and 0.050 μM, respectively, but neither of them inhibited EGFr autophosphorylation at 100 μM. We further investigated the profile of both compounds toward various tyrosine and serine/threonine kinases. The three compounds specifically inhibited PDGFr rather than the other kinases.
Synthesis, antimycobacterial activities and cytotoxicity on V79 of 3-[4′-Y-(1,1′-biphenyl)-4-yl]-N,N-dimethyl-3-(4-X-phenyl)-2- propen-1-amine derivatives
De Souza, Ana O,Santos Junior, Rubens R,Ferreira-Julio, Joao F,Rodriguez, Jaime A,Melo, Patricia S,Haun, Marcela,Sato, Daisy N,Duran, Nelson
, p. 843 - 850 (2007/10/03)
The derivatives of 3-(4′-bromo-[1,1′-biphenyl]-4-yl)-3-(4-X-phenyl)-N,N-dimethyl-2- propen-1-amine (5a-m) were synthesised through a Friedel-Crafts acylation followed by Wittig reaction. The effects of the compounds on standard strains of Mycobacterium sp. (ATCC) and M. tuberculosis isolated from clinical specimens were evaluated. Also the toxicity was determined on V79 cells line using neutral red uptake (NRU), nucleic acid content (NAC) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction to measure the cellular viability.
Synthesis and structure-activity relationships of benzophenone hydrazone derivatives with insecticidal activity
Boeger, Manfred,Duerr, Dieter,Gsell, Laurenz,Hall, Roger G.,Karrer, Friedrich,Kristiansen, Odd,Maienfisch, Peter,Pascual, Alfons,Rindlisbacher, Alfred
, p. 191 - 202 (2007/10/03)
A broad range of benzophenone hydrazone derivatives was prepared and tested against selected chewing insect pests, allowing the analysis of structure-activity relationships. Good activity was found only when the aromatic rings were substituted at the 4-positions with an halogen atom and a triflate or perhaloalkoxy group. In contrast, a number of substituents on the hydrazone part led to active compounds, the best results being achieved with acyl-type substituents. The excellent laboratory and greenhouse activity of the best representatives was confirmed in semi-field trials against Spodoptera littoralis. ° 2001 Society of Chemical Industry.
Antifungal agents. 10. Synthesis and antifungal activities of aryl-(1H-imidazol-1-yl)-(isoquinolin-1-yl) methane derivatives
Silvestri,Pagnozzi,Troccoli,Stefancich,Massa,Apuzzo,Perazzi,Artico,Simonetti
, p. 227 - 238 (2007/10/02)
Various aryl-(1H-imidazol-1-yl)-(isoquinolin-1-yl)methane derivatives have been synthesized and tested as antifungal agents. The new imidazoles have been obtained by the action of 1,1'-sulfinyldiimidazole on aryl-(isoquinolin-1-yl)carbinols, which have be
Syntheses of Asymmetrical Diaryl and Aryl Alkyl Ketones as Possible Non-steroidal Antiprogestational Agents
Kumar, Shiv,Seth, M.,Bhaduri, A. P.,Agnihotri, Anila,Srivastava, A. K.
, p. 154 - 157 (2007/10/02)
A number of asymmetrical diaryl and aryl alkyl ketones have been synthesised as possible non-steroidal antiprogestational agents.Evaluation of these compounds as competitive inhibitors of progesterone binding to uterine cytosol progesterone receptors of rabbit and human indicates that 3-methyl-4'-phenylbenzophenone (2) exhibits marginal activity in both the cases.However, this compound has been found to be inferior to R 5020 and d-norgestrel.
