- Crystal structure and supramolecular arrangement of heterochiral tripeptides
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The self-assembly properties of all possible stereoisomers of terminally protected Boc-Val-Phe-Phe-OMe, having sequence homogeneity with Alzheimer's amyloid-beta (Aβ18-20) peptide was investigated. The morphology analysis by field emission scan
- Dolai, Gobinda,Giri, Rajat Subhra,Roy, Sayanta,Mandal, Bhubaneswar
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- Effect of Stereochemistry on Chirality and Gelation Properties of Supramolecular Self-Assemblies
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Although chiral nanostructures have been fabricated at various structural levels, the transfer and amplification of chirality from molecules to supramolecular self-assemblies are still puzzling, especially for heterochiral molecules. Herein, four series o
- Qin, Minggao,Zhang, Yaqian,Xing, Chao,Yang, Li,Zhao, Changli,Dou, Xiaoqiu,Feng, Chuanliang
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p. 3119 - 3129
(2021/01/20)
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- On the Role of Chirality in Guiding the Self-Assembly of Peptides
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Homochirality in peptides is crucial in sustaining “like–like” intermolecular interactions that allow the formation of assemblies and aggregates and is ultimately responsible for the resulting material properties. With the help of a series of stereoisomer
- Basak, Shibaji,Singh, Ishwar,Ferranco, Annaleizle,Syed, Jebreil,Kraatz, Heinz-Bernhard
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supporting information
p. 13288 - 13292
(2017/10/07)
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- Design and synthesis of Hsp90 inhibitors: Exploring the SAR of Sansalvamide A derivatives
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Utilizing the structure-activity relationship we have developed during the synthesis of the first two generations and mechanism of action studies that point to the interaction of these molecules with the key oncogenic protein Hsp90, we report here the design of 32 new Sansalvamide A derivatives and their synthesis. Our new structures, designed from previously reported potent compounds, were tested for cytotoxicity on the HCT116 colon cancer cell line, and their binding to the biological target was analyzed using computational studies involving blind docking of derivatives using Autodock. Further, we show new evidence that our molecules bind directly to Hsp90 and modulate Hsp90's binding with client proteins. Finally, we demonstrate that we have integrated good ADME properties into a new derivative.
- Sellers, Robert P.,Alexander, Leslie D.,Johnson, Victoria A.,Lin, Chun-Chieh,Savage, Jeremiah,Corral, Ricardo,Moss, Jason,Slugocki, Tim S.,Singh, Erinprit K.,Davis, Melinda R.,Ravula, Suchitra,Spicer, Jamie E.,Oelrich, Jenna L.,Thornquist, Andrea,Pan, Chung-Mao,McAlpine, Shelli R.
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experimental part
p. 6822 - 6856
(2010/10/18)
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- Comprehensive study of sansalvamide A derivatives and their structure-activity relationships against drug-resistant colon cancer cell lines
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We report an extensive structure-activity relationship (SAR) of 62 compounds active against two drug-resistant colon cancer cell lines. Our comprehensive evaluation of two generations of compounds utilizes SAR, NMR, and molecular modeling to evaluate the
- Otrubova, Katerina,Lushington, Gerald,Vander Velde, David,McGuire, Kathleen L.,McAlpine, Shelli R.
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p. 530 - 544
(2008/09/18)
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- Synthesis of second-generation Sansalvamide A derivatives: Novel templates as potential antitumor agents
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We report the synthesis of 34 second-generation Sansalvamide A derivatives. San A derivatives have unique anticancer properties and target multiple cancers, including colon, pancreatic, breast, prostate, and melanoma. As novel templates, the derivatives d
- Rodriguez, Rodrigo A.,Pan, Po-Shen,Pan, Chung-Mao,Ravula, Suchitra,Lapera, Stephanie,Singh, Erinprit K.,Styers, Thomas J.,Brown, Joseph D.,Cajica, Julia,Parry, Emily,Otrubova, Katerina,McAlpine, Shelli R.
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p. 1980 - 2002
(2007/10/03)
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- Amine capture strategy for peptide bond formation by means of quinolinium thioester salts
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A new and unprecedented exploitation of quinolinium thioester salts 2 in peptide bond formation is reported. These synthetic tools were assessed during the preparation of a number of dipeptides 3a-f obtained in good yields with complete stereochemical integrity. A sequential mechanism related to a prior amine capture strategy is well-established. Additionally, a tripeptide 3g was prepared according to a "safety-catch" approach, thus demonstrating the important potential of these new synthetic tools in the design of new safety-catch linkers exploitable in Solid-Phase Peptide Synthesis (SPPS). Copyright
- Leleu, Stephane,Penhoat, Mael,Bouet, Alexis,Dupas, Georges,Papamicael, Cyril,Marsais, Francis,Levacher, Vincent
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p. 15668 - 15669
(2007/10/03)
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- Stereoselective reduction of N-hydroxy-α-iminocarbonyl-oligopeptide methyl esters with Zn-MsOH
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The reduction of N-hydroxy-α-imino esters with Zn-MsOH in THF afforded α-amino esters in high yields. The reduction of N-hydroxy-α-iminocarbonyl-oligopeptide methyl esters prepared from L-phenylalanine and L-leucine di-, tri-, tetrapeptides gave the corre
- Kise, Naoki,Takaoka, Shuji,Yamauchi, Masahiro,Ueda, Nasuo
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p. 7297 - 7300
(2007/10/03)
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- METHOD FOR STORING QUATERNARY AMMONIUM SALT
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A method of improving the stability of a quaternary ammonium salt and a method of efficiently preparing the quaternary ammonium salt having improved stability.
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- Synthesis of a reported calpain inhibitor isolated from Streptomyces griseus
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The reported diketopiperazine calpain inhibitor, cis-L-L-3,6-bis-(4-hydroxybenzyl)-1,4-dimethylpiperazine-2,5-dione 1, and its analogues 3 and 4 were synthesized from the corresponding amino acids. The previously assigned structure of 1 is confirmed but n
- Donkor,Sanders, M. Lee
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p. 2647 - 2649
(2007/10/03)
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