34107-46-5Relevant articles and documents
Picazoplatin, an azide-containing platinum(II) derivative for target analysis by click chemistry
White, Jonathan D.,Osborn, Maire F.,Moghaddam, Alan D.,Guzman, Lindsay E.,Haley, Michael M.,DeRose, Victoria J.
, p. 11680 - 11683 (2013)
Despite the broad use of platinum-based chemotherapeutics, identification of their full range of cellular targets remains a significant challenge. In order to identify, visualize, and isolate cellular targets of Pt(II) complexes, we have modified the chemotherapeutic drug picoplatin with an azide moiety for subsequent click reactivity. The new compound picazoplatin readily binds DNA and RNA oligonucleotides and undergoes facile post-labeling click reactions to alkyne-fluorophore conjugates. Pt-fluorophore click reactions in rRNA purified from drug-treated Saccharomyces cerevisiae demonstrate its potential for future in vivo efforts.
An Open Drug Discovery Competition: Experimental Validation of Predictive Models in a Series of Novel Antimalarials
?eren, Mario,Aithani, Laksh,Anderson, Mark,Cardoso-Silva, Jonathan,Cincilla, Giovanni,Conduit, Gareth J.,Galushka, Mykola,Guan, Davy,Hallyburton, Irene,Irwin, Benedict W. J.,Kirk, Kiaran,Lehane, Adele M.,Lindblom, Julia C. R.,Lui, Raymond,Matthews, Slade,McCulloch, James,Motion, Alice,Ng, Ho Leung,Robertson, Murray N.,Spadavecchio, Vito,Tatsis, Vasileios A.,Todd, Matthew H.,Tse, Edwin G.,Van Hoorn, Willem P.,Wade, Alexander D.,Whitehead, Thomas M.,Willis, Paul
supporting information, p. 16450 - 16463 (2021/11/24)
The Open Source Malaria (OSM) consortium is developing compounds that kill the human malaria parasite, Plasmodium falciparum, by targeting PfATP4, an essential ion pump on the parasite surface. The structure of PfATP4 has not been determined. Here, we des
Ruthenium-catalyzed ester reductions applied to pharmaceutical intermediates
Shaalan, Youssef,Boulton, Lee,Jamieson, Craig
supporting information, p. 2745 - 2751 (2020/11/30)
Ruthenium pincer complexes were synthesized and used for catalytic ester reductions under mild conditions (～5 bar of hydrogen). An experimental design approach was used to optimize the conditions for yield, purity, and robustness. Evidence for the catalytically active ruthenium dihydride species is presented. Observed intermediates and side products, as well as time-course data, were used to build mechanistic insight. The optimized procedure was further demonstrated through scaled-up reductions of two pharmaceutically relevant esters, both in batch and continuous flow.
Iron catalysed selective reduction of esters to alcohols
Tamang, Sem Raj,Cozzolino, Anthony F.,Findlater, Michael
supporting information, p. 1834 - 1838 (2019/02/20)
The reaction of (dppBIAN)FeCl2 with 3 equivalents of n-BuLi affords a catalytically active anionic Fe complex; the nature of the anionic complex was probed using EPR and IR experiments and is proposed to involve a dearomatized, radical, ligand scaffold. This complex is an active catalyst for the hydrosilylation of esters to afford alcohols; loadings as low as 1 mol% were employed.
HETEROCYCLIC INHIBITORS OF PCSK9
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Page/Page column 100; 101; 102, (2018/10/24)
This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I): (I) wherein A, D and Q are described herein.
Modular Route to Azaindanes
Huang, Qi,Zard, Samir Z.
supporting information, p. 3895 - 3898 (2017/07/26)
A convergent radical based route to azaindanes is described, relying on the degenerative addition transfer of various substituted S-(pyridylmethyl)-O-ethyl dithiocarbonates (xanthates) to functional alkenes followed by radical cyclization onto the pyridine ring activated by protonation with trifluoroacetic acid. In one case, a richly decorated cyclohepta[b]pyridine could be assembled swiftly by allowing the first adduct to N-phenylmaleimide to undergo addition to N-allylphthalimide prior to cyclization.
P2X3 AND/OR P2X2/3 COMPOUNDS AND METHODS
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Paragraph 0152; 0155; 0156, (2015/07/07)
The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient.
PROTEIN KINASE INHIBITORS
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Paragraph 0181, (2015/07/15)
The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
SPIROHYDANTOIN COMPOUNDS AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS
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Page/Page column 80; 81, (2013/09/12)
The present invention relates to a compound of formula (1-1 ) in free form or in pharmaceutically acceptable salt form in which the substituents are as defined in the specification; to its preparation, to its use as a medicament and to medicaments comprising it. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
PROTEIN KINASE INHIBITORS
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Page/Page column 58-59, (2014/01/07)
The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
