33918-15-9Relevant academic research and scientific papers
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 001925-001927, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 4203; 4204, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
Stereoselective Synthesis of Isochromanones by an Asymmetric Ortho-Lithiation Strategy: Synthetic Access to the Isochromanone Core of the Ajudazols
Essig, Sebastian,Menche, Dirk
, p. 1943 - 1966 (2016/03/15)
Full details on the design, development, and application of a highly stereoselective strategy for the synthesis of isochromanones are reported. The method is based on an asymmetric ortho lithiation with aldehyde electrophiles and utilizes the chiral memor
Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90
He, Huazhong,Zatorska, Danuta,Kim, Joungnam,Aguirre, Julia,Llauger, Laura,She, Yuhong,Wu, Nian,Immormino, Robert M.,Gewirth, Daniel T.,Chiosis, Gabriela
, p. 381 - 390 (2007/10/03)
Hsp90 is a chaperone protein that allows cancer cells to tolerate the many components of dysregulated pathways. Its inactivation may result in targeting multiple molecular alterations and, thus, in reverting the transformed phenotype. The PU-class, a purine-scaffold Hsp90 inhibitor series, has been reported to be potent and selective against Hsp90 both in vitro and in vivo models of cancer. Here, a series of this class was synthesized and evaluated as inhibitors of the chaperone. The structure-activity relationship and selectivity for tumor Hsp90 of compounds within the series is presented. The study identifies water soluble derivatives (> 5 mM in PBS pH 7.4) of nanomolar potency (IC50 ~ 50 nM) in cellular and animal models of cancer. Binding affinities of these compounds for Hsp90 correlate well with their biological activities. When administered in vivo to mice bearing MDA-MB-468 human breast cancer xenografted tumors, these agents result in pharmacologically relevant concentrations and, accordingly, in modulation of Hsp90-client proteins in tumors.
SMALL-MOLECULE HSP90 INHIBITORS
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Page/Page column 30, (2008/06/13)
Hsp90 inhibitors havin are rovided havin the formula: (I) with a 2',4',5'-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4' and 5' positions on the aryl group, wherei
Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents
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Example 6, (2008/06/13)
Antiatherosclerotic agents are provided having the following structure: wherein: R1is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenylalkyl of 7-10 carbon atoms; and R2, R3, R4, R5, and R6are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy of 6-12 carbon atoms, aralkyloxy of 7-12 carbon atoms, fluoroalkoxy of 1-6 carbon atoms, trifluoromethyl, alkylthio of 1-3 carbon atoms, alkylsulfonyl of 1-3 carbon atoms, —SCF3, nitro, alkylamino in which the alkylamino moiety has 1-6 carbon atoms, or dialkylamino in which each alkyl group has 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
SIMPLE SYNTHESIS OF 3-(N-ALKYLAMINO)-1-PROPANOLS
Artyushin, O. I.,Petrovskii, P. V.,Mastryukova, T. A.,Kabachnik, M. I.
, p. 1911 - 1913 (2007/10/02)
Various 3-(N-alkylamino)-1-propanols were obtained by the lithium aluminum hydride reduction of the products of the reaction of 3-amino-1-propanol with carbonyl compounds.This method for the synthesis of aminopropanols is applicable in the case of optimal electrophilicity of the carbonyl component.
The Conformational Analysis of Saturated Heterocycles. Part 100. 1-Oxa-3-azacyclohexanes
Katritzky, Alan R.,Baker, Victor J.,Brito-Palma, Fernando M. S.
, p. 1739 - 1745 (2007/10/02)
Conformational equilibria and barriers to ring and nitrogen inversion are determined by 1H and 13C n.m.r. for 13 1-oxa-3-azacyclohexanes and correlated with recent work on the conformational analysis of saturated heterocycles.
