99359-33-8Relevant academic research and scientific papers
Specific Inhibitor of Placental Alkaline Phosphatase Isolated from a DNA-Encoded Chemical Library Targets Tumor of the Female Reproductive Tract
Bassi, Gabriele,Cazzamalli, Samuele,Favalli, Nicholas,Manz, Markus G.,Neri, Dario,Onda, Yuichi,Pellegrino, Christian,Scheuermann, J?rg
supporting information, p. 15799 - 15809 (2021/11/16)
Placental alkaline phosphatase (PLAP) is an abundant surface antigen in the malignancies of the female reproductive tract. Nevertheless, the discovery of PLAP-specific small organic ligands for targeting applications has been hindered by ligand cross-reac
ANTIMICROBIAL COMPOUNDS AND METHODS
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Paragraph 00816, (2020/07/31)
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
Design, Synthesis, and Cytotoxic Activity of 3-Aryl-N-hydroxy-2-(sulfonamido)propanamides in HepG2, HT-1080, KB, and MCF-7 Cells
Shao, Duanyang,Zhang, Guo-Ning,Niu, Weixiao,Li, Ziqiang,Zhu, Mei,Wang, Juxian,Li, Donghui,Wang, Yucheng
, (2019/04/03)
A new series of (sulfonamido)propanamides (6a1–6a13, 6b1–6b15, 7c1–7c5, 6d1–6d5, 6e1–6e6) was designed and synthesized. All the synthesized compounds were characterized by NMR and mass spectrometry. The target compounds were evaluated for their in vitro c
TETRAHYDROISOQUINOLINES AS PRMT5 INHIBITORS
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Page/Page column 96, (2017/09/27)
A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from the group consisiting of H, halo, C1-4 alkoxy, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH-C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl; wherein when R2e is H, at least one of R1a, R1b, R1c and R1d is selected from C1-4 alkoxy, C2-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH-C1-4 alkyl and cyano.
Suzuki-Miyaura Diversification of Amino Acids and Dipeptides in Aqueous Media
Willemse, Tom,Van Imp, Karolien,Goss, Rebecca J. M.,Van Vlijmen, Herman W. T.,Schepens, Wim,Maes, Bert U. W.,Ballet, Steven
, p. 2055 - 2070 (2015/11/24)
The Suzuki-Miyaura derivatisation of free amino acids, peptides and proteins is an attractive area with considerable potential utility for medicinal chemistry and chemical biology. Here we report the modification of unprotected and Boc-protected aromatic amino acids and dipeptides in aqueous media, enabling heteroarylation and vinylation. We systematically investigate the impact of the peptide backbone and adjacent amino acid residues upon the reaction. Our studies reveal that although asparagine and histidine hinder the reaction, by utilising dppf, a ferrocene-based bidentate phosphine ligand, cross coupling of halophenylalanine or halotryptophan adjacent to such a residue could be enabled. Our studies reveal dppf to have good compatibility with all unprotected, proteinogenic amino acid side chains.
Studies Toward the Total Synthesis and Stereochemical Assignment of Microspinosamide
Santhakumar, Gajan,Payne, Richard J.
, p. 1885 - 1889 (2015/12/26)
Efforts toward the total synthesis and stereochemical assignment of the cyclic depsipeptide natural product microspinosamide are described. A single diastereoisomer was targeted corresponding to the predicted structure of the natural product incorporating a (2S, 3R)-β-hydroxy-p-bromophenylalanine residue. Assembly was achieved through the initial synthesis of a cyclic depsipeptide and a linear peptide thioester fragment by solid-phase peptide synthesis, followed by fusion of the two fragments through a native chemical ligation-oxidation protocol. Extensive spectroscopic analysis showed structural differences to the isolated natural product, suggesting that a diastereoisomer of microspinosamide had been synthesised. This work lays the foundation for the future synthesis of the correct diastereoisomer.
Effect of the 4′-substituted phenylalanine moiety of sansalvamide A peptide on antitumor activity
Liu, Shouxin,Yang, Yihua,Zhao, Cuiran,Huang, Jing,Han, Chunyu,Han, Jianrong
, p. 463 - 467 (2014/04/17)
Eight sansalvamide A peptide analogues with 4′-fluoride, 4′-chloride, 4′-bromide, 4′-iodide, and 4′- methoxyphenylalanine moieties were synthesized. The effect of these para-substitutions of sansalvamide A peptide on their cytotoxicity was evaluated using HCT-116, MDA-MB-231, HT-29, HCT-15, K562, HeLa, and A549 cell lines. The 4′-methoxyphenylalanine analog of sansalvamide A peptide was found to be a promising antitumor agent.
PEPTIDYL NITRILCOMPOUNDS AS PEPTIDASE INHIBITORS
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Page/Page column 118, (2012/09/22)
The invention relates to compounds of Formula (II) and their use in theraphy as peptidase inhibitors.
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes
N?teberg, Daniel,Hamelink, Elizabeth,Hultén, Johan,Wahlgren, Mats,Vrang, Lotta,Samuelsson, Bertil,Hallberg, Anders
, p. 734 - 746 (2007/10/03)
A series of protease inhibitors targeted at the malarial enzymes plasmepsin I and II, and encompassing a basic hydroxyethylamine transition state isostere scaffold, was prepared. The substituents in the P1′ position were varied and the biological activiti
