88987-42-2Relevant academic research and scientific papers
Platinum(II) Complexes of Functionalized Malonato Ligands: Unequivocal Synthesis, Interaction with a Tetradeoxyribonucleotide and Deoxyribonucleic Acid
Laurent, Jean-Pierre,Morvan, Bernard
, p. 2141 - 2146 (1993)
The unequivocal syntheses of four cis-> complexes has been achieved, avoiding any interaction between the pendant carboxyl group and the platinum.The complexes have been characterized by elemental analysis, 13C NMR and FAB mass spectroscopy.Their interaction with a tetradeoxyribonucleotide d(T-G-G-T) (G = guanosine, T = ribosylthymine) and DNA (in vitro) has been investigated to show that they form adducts of the type 7,N7'>> as do the known therapeutically activeplatinum complexes.However, the presence of the free carbonyl function increases significantly the reactivity with respect to that of the non-functionalized malonato complexes >.
PROTAC-mediated crosstalk between E3 ligases
Steinebach, Christian,Kehm, Hannes,Lindner, Stefanie,Vu, Lan Phuong,K?pff, Simon,López Mármol, álvaro,Weiler, Corinna,Wagner, Karl G.,Reichenzeller, Michaela,Kr?nke, Jan,Gütschow, Michael
supporting information, p. 1821 - 1824 (2019/02/12)
Small-molecule heterobifunctional degraders can effectively control protein levels and are useful research tools. We assembled proteolysis targeting chimeras (PROTACs) from a cereblon (CRBN) and a von-Hippel-Lindau (VHL) ligase ligand and demonstrated a PROTAC-induced heterodimerization of the two E3 ligases leading to unidirectional and efficient degradation of CRBN.
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
Hu, Jiantao,Hu, Biao,Wang, Mingliang,Xu, Fuming,Miao, Bukeyan,Yang, Chao-Yie,Wang, Mi,Liu, Zhaomin,Hayes, Daniel F.,Chinnaswamy, Krishnapriya,Delproposto, James,Stuckey, Jeanne,Wang, Shaomeng
, p. 1420 - 1442 (2019/01/30)
The estrogen receptor (ER) is a validated target for the treatment of estrogen receptor-positive (ER+) breast cancer. Here, we describe the design, synthesis, and extensive structure-activity relationship (SAR) studies of small-molecule ERα degraders base
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
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Paragraph 001036, (2019/01/08)
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
Tri-Orthogonal Scaffolds for the Solid-Phase Synthesis of Peptides
Pícha, Jan,Fabre, Benjamin,Budě?ínsky, Milo?,Hajduch, Jan,Abdellaoui, Mehdi,Jirá?ek, Ji?í
supporting information, p. 5180 - 5192 (2018/08/01)
Multi-orthogonal scaffolds can be useful for the attachment of several different compounds to the same central skeleton. Such compounds can find applications in the development of protein mimics because of their potential to mimic several distant epitopes
INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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Paragraph 670; 671, (2016/10/11)
The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
OLIGONUCLEOTIDE-LIGAND CONJUGATES AND PROCESS FOR THEIR PREPARATION
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Page/Page column 182; 183, (2015/02/02)
The present invention relates to ligand conjugates of oligonucleotides (e.g., iRNA agents) and methods for their preparation. The ligands are derived primarily from monosaccharides These conjugates are useful for the in vivo delivery of oligonucleotides.
Heterovalent inhibitors targeting N-end Rule Pathway and its use
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Paragraph 0145; 0146, (2016/10/10)
An alkali-soluble polymer resin compound of formula 1 a including N-end Rule pathway inhibitors disclosure the composition. According to type 1 and type 2 herein each compounds recognizing substrate UBR box and a ClpS box a mammal having two tolerance N-e
The development of a new class of inhibitors for betaine-homocysteine S-methyltransferase
Pi?ha, Jan,Vaňek, Václav,Budě??sińsky, Milo?,Mlad?ková, Jana,Garrow, Timothy A.,Ji??acek, Ji??i
, p. 256 - 275 (2013/10/01)
Betaine-homocysteine S-methyltransferase (BHMT) is an important zinc-dependent methyltransferase that uses betaine as the methyl donor for the remethylation of homocysteine to form methionine. In the liver, BHMT performs to half of the homocysteine remethylation. In this study, we systematically investigated the tolerance of the enzyme for modifications at the "homocysteine" part of the previously reported potent inhibitor (R,S)-5-(3-amino-3-carboxy-propylsulfanyl)-pentanoic acid (1). In the new compounds, which are S-alkylated homocysteine derivatives, we replaced the carboxylic group in the "homocysteine" part of inhibitor 1 with different isosteric moieties (tetrazole and oxadiazolone); we suppressed the carboxylic negative charge by amidations; we enhanced acidity by replacing the carboxylate with phosphonic or phosphinic acids; and we introduced pyrrolidine steric constraints. Some of these compounds display high affinity toward human BHMT and may be useful for further pharmacological studies of this enzyme. Although none of the new compounds were more potent inhibitors than the reference inhibitor 1, this study helped to completely defi ne the structural requirements of the active site of BHMT and revealed the remarkable selectivity of the enzyme for homocysteine.
A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
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Page/Page column 50, (2008/06/13)
The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
