37470-83-0Relevant academic research and scientific papers
Convenient synthesis of an isoxazole compound, KRIBB3, as an anticancer agent
Lee, Hyeong Kyu,Yun, Eunju,Min, Ji Hye,Yoon, Kab Seog,Choung, Dong-Ho,Lee, Sangku
experimental part, p. 1890 - 1894 (2012/06/04)
A diaryl isoxazole compound, KRIBB3, which exhibits strong antimigratory and antimitotic activities against cancer cells, was prepared in a practical synthetic way. The synthetic method may provide easy access to KRIBB3 analogs with various substituents a
Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90
O'Boyle, Niamh M.,Knox, Andrew J.S.,Price, Trevor T.,Williams, D. Clive,Zisterer, Daniela M.,Lloyd, David G.,Meegan, Mary J.
experimental part, p. 6055 - 6068 (2011/11/06)
Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical trials and represent a new and exciting area in the treatment of cancer. Heat shock protein 90 inhibitors have huge structural diversity, and here we present the lead identification of novel inhibitors based on β-lactam and imine templates. β-Lactam 5 and imines 12 and 18 exhibit binding to heat shock protein 90-α with IC50 values of 5.6 μM, 14.5 μM, and 22.1 μM, respectively. The binding affinity displayed by these compounds positions them as lead compounds for the design of future inhibitors of heat shock protein 90 based on the β-lactam and imine templates.
Design, synthesis, and structure - Activity relationships for chimeric inhibitors of Hsp90
Shen, Gang,Wang, Mingwen,Welch, Timothy R.,Blagg, Brian S. J.
, p. 7618 - 7631 (2007/10/03)
(Chemical Equation Presented) Inhibition of the 90 kDa heat shock protein (Hsp90) family of molecular chaperones represents a promising new chemotherapeutic approach toward the treatment of several cancers. Previous studies have demonstrated that the natural products, radicicol and geldanamycin, are potent inhibitors of the Hsp90 N-terminal ATP binding site. The cocrystal structures of these molecules bound to Hsp90 have been determined, and through molecular modeling and superimposition of these ligands, hybrids of radicicol and geldanamycin have been designed. A series of macrocylic chimeras of radicicol and geldanamycin and the corresponding seco-agents have been prepared and evaluated for both antiproliferative activity and their ability to induce Hsp90-dependent client protein degradation.
NEW DIARYL-ISOXAZOLE DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME FOR THE PREVENTION AND THE TREATMENT OF CANCERS
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Page/Page column 10-11, (2010/11/25)
The present invention relates to new diaryl-isoxazole derivatives, and pharmaceutical compositions containing the same as an effective ingredient for the prevention and the treatment of cancers. Diaryl-isoxazole derivatives of the present invention inhibi
Pharmaceutical compositions of diaryl-isoxazole derivatives for the prevention and treatment of cancers
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Page/Page column 3-4, (2010/02/12)
The present invention relates to a pharmaceutical composition for the prevention and the treatment of cancers containing diaryl-isoxazole derivatives as an effective ingredient. Diaryl-isoxazole derivatives of the present invention inhibit metastasis of b
DERIVATIVES OF CHROMEN-2-ONE AS INHIBITORS OF VEGF PRODUCTION IN MAMMALIAN CELLS
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Page 69, (2008/06/13)
The compounds of formula (I) wherein A and R1-R5 are as defined in the description, are inhibitors of Vascular Endothelial Growth Factor and are useful as angiogenesis inhibitors and antiproliferative agents.
USE OF PLA2 INHIBITORS AS TREATMENT FOR ALZHEIMER'S DISEASE
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, (2008/06/13)
This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of phospholipase A2. This invention also provides a series of compounds which are useful as inhibitors of phospholipases A2, especially cytosolic phospholipase A2.
1,2,4-TRIOXYGENATED BENZENE DERIVATIVES USEFUL AS LEUKOTRIENE ANTAGONISTS
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, (2008/06/13)
This invention provides 1,2,4-trioxygenated benzene derivatives which are leukotriene B 4 antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
