719288-40-1Relevant academic research and scientific papers
Screening of a virtual mirror-image library of natural products
Noguchi, Taro,Oishi, Shinya,Honda, Kaori,Kondoh, Yasumitsu,Saito, Tamio,Ohno, Hiroaki,Osada, Hiroyuki,Fujii, Nobutaka
, p. 7653 - 7656 (2016)
We established a facile access to an unexplored mirror-image library of chiral natural product derivatives using d-protein technology. In this process, two chemical syntheses of mirror-image substances including a target protein and hit compound(s) allow the lead discovery from a virtual mirror-image library without the synthesis of numerous mirror-image compounds.
P-Hydroxyphenacyl photoremovable protecting groups Robust photochemistry despite substituent diversity
Givens, Richard S.,Stensrud, Kenneth,Conrad, Peter G.,Yousef, Abraham L.,Perera, Chamani,Senadheera, Sanjeewa N.,Heger, Dominik,Wirz, Jakob
scheme or table, p. 364 - 384 (2011/06/22)
A broadly based investigation of the effects of a diverse array of substituents on the photochemical rearrangement of p-hydroxyphenacyl esters has demonstrated that common substituents such as F, MeO, CN, CO2R, CONH2, and CH3 have little effect on the rate and quantum efficiencies for the photo-Favorskii rearrangement and the release of the acid leaving group or on the lifetimes of the reactive triplet state. A decrease in the quantum yields across all substituents was observed for the release and rearrangement when the photolyses were carried out in buffered aqueous media at pHs that exceeded the ground-state pKa of the chromophore where the conjugate base is the predominant form. Otherwise, substituents have only a very modest effect on the photoreaction of these robust chromophores.
4-Amino derivatives of the Hsp90 inhibitor CCT018159
Barril, Xavier,Beswick, Mandy C.,Collier, Adam,Drysdale, Martin J.,Dymock, Brian W.,Fink, Alexandra,Grant, Kate,Howes, Robert,Jordan, Allan M.,Massey, Andrew,Surgenor, Allan,Wayne, Joanne,Workman, Paul,Wright, Lisa
, p. 2543 - 2548 (2007/10/03)
Novel piperazinyl, morpholino and piperidyl derivatives of the pyrazole-based Hsp90 inhibitor CCT018159 are described. Structure-activity relationships have been elucidated by X-ray co-crystal analysis of the new compounds bound to the N-terminal domain o
PYRAZOLE COMPOUNDS
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Page 54-55, (2008/06/13)
Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted Cl-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or Cl-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r (Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -S02-, -C(=O)O-, -OC(=O)-, -NW-, -C(=O)NRA-, -NRAC(=O)-, -SO2NRA- , or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.
