133232-56-1Relevant articles and documents
METHOD FOR PRODUCING HALOGENATED BENZENE DERIVATIVE
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Paragraph 0075; 0076; 0077; 0078; 0079; 0080; 0081-0088, (2018/06/30)
PROBLEM TO BE SOLVED: To provide a method for producing a halogenated benzene derivative, which is highly efficient and economically advantageous. SOLUTION: The method produces a halogenated benzene derivative represented by formula (2) by reacting a benzene derivative represented by formula (1) with a halogenating agent selected from N-halogen succinimide and the like in the presence of an acid selected from sulfuric acid and methanesulfonic acid. (R1 is H, a hydroxyl group, or an alkoxy group; R2 and R3 are each independently H or a hydrocarbon group; a is an integer of 1-4; b is an integer of 1-4; a+b is an integer of 2-5; X is a halogen atom; c is an integer of 1-4; and a+b+c is an integer of 3-6). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone
Kung, Pei-Pei,Funk, Lee,Meng, Jerry,Collins, Michael,Zhou, Joe Zhongxiang,Catherine Johnson,Ekker, Anne,Wang, Jeff,Mehta, Pramod,Yin, Min-Jean,Rodgers, Caroline,Davies II, Jay F.,Bayman, Eileen,Smeal, Tod,Maegley, Karen A.,Gehring, Michael R.
supporting information; experimental part, p. 6273 - 6278 (2009/08/15)
Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC50 values averaging 20 nM.
AMIDE RESORCINOL COMPOUNDS
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Page/Page column 41; 108, (2008/06/13)
The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.