- PEPTIDE-OLIGOUREA HYBRID COMPOUNDS
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The present description relates to peptidomimetic foldamers, and their synthesis. In particular, the description provides peptide-amino urea hybrid peptidomimetic foldamers comprising an alpha amino acid peptide portion and an oligourea portion.
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Paragraph 00287-00289
(2020/07/31)
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- METHOD FOR PREPARING SULFONAMIDES DRUGS
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Provided is a method for preparing sulfonamides which are inhibitors of Bcl-2/ Bcl-xL, comprising the compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorophenyl) -1-isopropyl-4-methylsulfonyl-5-methyI-1H-pyrrol-3-yl)-5-fluorophenyl)piperazin-1-yI)-phenylam inosulf
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Page/Page column 41; 45
(2020/07/21)
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- Process for preparing sulfonamide compounds
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The invention relates to a process for preparing sulfonamide compounds. The sulfonamide compound is an inhibitor of Bcl-2/Bcl-xL and is prepared from a compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorphenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrole-3-yl
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Paragraph 0415; 0453-0456; 0494; 0579-0582
(2020/07/24)
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- PROCESS FOR PREPARING SULFONAMIDE COMPOUNDS
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Provided are a process for preparing a sulfonamide compound which is an inhibitor of Bcl-2/Bcl-xL, including the compound (3R) -1- (3- (4- (4- (4- (3- (2- (4-chlorophenyl) -1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl) -5-fluorophenyl) piperazine
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Page/Page column 69-70
(2020/09/03)
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- iSPAAC: Isomer-Free Generation of a Bcl-xL-Inhibitor in Living Cells
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Strain-promoted azide–alkyne cycloadditions (SPAAC) have proven extremely useful for labeling of biomolecules, but typically produce isomeric mixtures. This is not appropriate for the formation of bioactive molecules in living cells. Here, the first use o
- Lis, Christian,Rubner, Stefan,Gr?st, Corinna,Hoffmann, Ralf,Knappe, Daniel,Berg, Thorsten
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supporting information
p. 13762 - 13766
(2018/09/14)
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- APOPTOSIS-INDUCING AGENTS
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Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti apoptotic Bcl-xL protein.
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Page/Page column 118
(2014/03/22)
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- Profiling small molecule inhibitors against helix-receptor interactions: The Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2
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We validate a practical methodology for the rapid profiling of small molecule inhibitors of protein-protein interactions. We find that a well known BH3 family inhibitor can potently inhibit the p53/hDM2 interaction.
- Porter, Jason R.,Helmers, Mark R.,Wang, Ping,Furman, Jennifer L.,Joy, Stephen T.,Arora, Paramjit S.,Ghosh, Indraneel
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supporting information; experimental part
p. 8020 - 8022
(2011/01/03)
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- BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES
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Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
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Page/Page column 287
(2010/06/20)
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- DMSO-aided o-iodoxybenzoic acid (IBX) oxidation of Fmoc-protected amino alcohols
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A fast and highly convenient procedure for the formation of Fmoc-protected amino aldehydes from the corresponding alcohols using 1.1 equiv. of IBX in the presence of dimethylsulfoxide (DMSO) is discussed. This procedure leads to the clean synthesis of Fmo
- Chen, Jack J.,Aduda, Vince
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p. 3493 - 3499
(2008/03/13)
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- Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo
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Development of a rationally designed potentiator of cancer chemotherapy, via inhibition of Bcl-XL function, is described. Lead compounds generated by NMR screening and directed parallel synthesis displayed sub-μM binding but were strongly deactivated in the presence of serum. The dominant component of serum deactivation was identified as domain III of human serum albumin (HSA); NMR solution structures of inhibitors bound to both Bcl-X L and HSA domain III indicated two potential optimization sites for separation of affinities. Modifications at both sites resulted in compounds with improved Bcl-XL binding and greatly increased activity in the presence of human serum, culminating in 73R, which bound to Bcl-XL with a Ki of 0.8 μM. In a cellular assay 73R reversed the protection afforded by Bcl-XL overexpression against cytokine deprivation in FL5.12 cells with an EC50 of 0.47 μM. 73R showed little effect on the viability of the human non small cell lung cancer cell line A549. However, consistent with the proposed mechanism, 73R potentiated the activity of paclitaxel and UV irradiation in vitro and potentiated the antitumor efficacy of paclitaxel in a mouse xenograft model.
- Wendt, Michael D.,Shen, Wang,Kunzer, Aaron,McClellan, William J.,Bruncko, Milan,Oost, Thorsten K.,Ding, Hong,Joseph, Mary K.,Zhang, Haichao,Nimmer, Paul M.,Ng, Shi-Chung,Shoemaker, Alexander R.,Petros, Andrew M.,Oleksijew, Anatol,Marsh, Kennan,Bauch, Joy,Oltersdorf, Tilman,Belli, Barbara A.,Martineau, Darlene,Fesik, Stephen W.,Rosenberg, Saul H.,Elmore, Steven W.
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p. 1165 - 1181
(2007/10/03)
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- N-acylsulfonamide apoptosis promoters
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N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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- N-Acylsulfonamide apoptosis promoters
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N-Benzoyl arylsulfonamides having the formula Are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
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- Chiral N-Protected β-Iodoamines from α-Aminoacids: a General Synthesis
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N-Protected D- or L-β-iodoamines (as 2), which are useful intermediates for the preparation of chiral β-aminoacids, are obtained smoothly from β-aminols (as 1) in two steps and high yields.
- Caputo, Romualdo,Cassano, Ersilia,Longobardo, Luigi,Palumbo, Giovanni
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p. 167 - 168
(2007/10/02)
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