94670-76-5Relevant articles and documents
Asymmetric C–H activation as a modern strategy towards expedient synthesis of steganone
Dherbassy, Quentin,Wencel-Delord, Joanna,Colobert, Fran?oise
, p. 5238 - 5245 (2016)
A formal synthesis of (+)-steganone by means of atroposelective C–H activation is reported. The herein described strategy is very straightforward as the targeted scaffold is afforded in only 10 steps, amongst which five of them are conducted without isola
Heteroatom-containing novel high B-ring berberine analogues and C-H activation synthesis method thereof
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Paragraph 0011; 0014-0015, (2020/11/02)
The invention provides a heteroatom-containing novel high B-ring berberine analogue and a C-H activation synthesis method thereof. The novel high-B-ring berberine analogue with the potential p300 histone acetyltransferase inhibitory activity is prepared f
Fused Amino Pyridines for the Treatment of Lung Cancer
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Paragraph 0149, (2016/11/17)
The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.
Access to Atropisomerically En-riched Biaryls by the Coupling of Aryllithiums with Arynes under Control by Homochiral Oxazolines
Yalcouye, Boubacar,Berthelot-Bréhier, Ana?s,Augros, David,Panossian, Armen,Choppin, Sabine,Chessé, Matthieu,Colobert, Fran?oise,Leroux, Frédéric R.
supporting information, p. 725 - 732 (2017/01/18)
We report the preparation of axially stereoenriched biphenyls by the coupling of in situ generated aryllithiums and arynes using chiral oxazoline auxiliaries. The design of the aryne precursors, the choice of oxazoline and the reaction conditions were key to accessing the desired, highly substituted, atropisomerically enriched biarylic products. In one case, the two atropo-diastereomers could be obtained in isomerically pure form by column chromatographic separation and their absolute configurations established by X-ray crystallography. The stereoselectivity of the reaction seems to be governed by subtle parameters.
Atropo-diastereoselective coupling of aryllithiums and arynes — variations around the chiral auxiliary
Augros, David,Yalcouye, Boubacar,Berthelot-Bréhier, Ana?s,Chessé, Matthieu,Choppin, Sabine,Panossian, Armen,Leroux, Frédéric R.
, p. 5208 - 5220 (2016/08/02)
The atropo-selective coupling of in situ generated arynes and aryllithiums bearing various chiral auxiliaries ortho to lithium (tert-butylsulfoxide, para-tolylsulfoxide, tartrate-derived chiral diethers and oxazolines) is described. Chiral oxazolines showed the best results in terms of yields of coupling products. Different reaction parameters like the nature of the aryne precursor, the oxazoline, the alkyllithium base or the solvent revealed to be crucial for obtaining good yields and for diastereoselection.
FUSED AMINO PYRIDINES FOR THE TREATMENT OF BRAIN TUMORS
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, (2010/08/07)
The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.
HSP90 Inhibitors Containing a Zinc Binding Moiety
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Page/Page column 36, (2008/12/08)
The present invention relates to HSP90 inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
FUSED AMINO PYRIDINE AS HSP90 INHIBITORS
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Page/Page column 38, (2008/12/08)
The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
PtCl2-catalyzed hydrative cyclization of trialkyne functionalities to form bicyclic spiro ketones
Chang, Hsu-Kai,Datta, Swarup,Das, Arindam,Odedra, Arjan,Liu, Rai-Shung
, p. 4744 - 4747 (2008/02/08)
(Chemical Equation Presented) Triple rounds: A regioselective hydrative cyclization of triynes has been developed to give bicyclic β-hydroxy spiro ketones, which undergo subsequent dehydration to give the β,γ- unsaturated ketones (see scheme). Model reactions suggest that this platinum catalysis includes two selective hydrations, an alkyne insertion, and an aldol condensation.
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.