136027-16-2Relevant academic research and scientific papers
Sulfono-γ-AA modified peptides that inhibit HIV-1 fusion
Bolarinwa, Olapeju,Zhang, Meng,Mulry, Erin,Lu, Min,Cai, Jianfeng
, p. 7878 - 7882 (2018)
The utilization of bioactive peptides in the development of highly selective and potent pharmacological agents for the disruption of protein-protein interactions is appealing for drug discovery. It is known that HIV-1 entry into a host cell is through a f
Probing the structural requirements of peptoids that inhibit HDM2-p53 interactions
Hara, Toshiaki,Durell, Stewart R.,Myers, Michael C.,Appella, Daniel H.
, p. 1995 - 2004 (2006)
Many cellular processes are controlled by protein-protein interactions, and selective inhibition of these interactions could lead to the development of new therapies for several diseases. In the area of cancer, overexpression of the protein, human double minute 2 (HDM2), which binds to and inactivates the protein p53, has been linked to tumor aggressiveness and drug resistance. In general, inhibition of protein-protein interactions with synthetic molecules is challenging and currently remains a largely uncharted area for drug development. One strategy to create inhibitors of protein-protein interactions is to recreate the three-dimensional arrangement of side chains that are involved in the binding of one protein to another, using a nonnatural scaffold as the attachment point for the side chains. In this study, we used oligomeric peptoids as the scaffold to begin to develop a general strategy in which we could rationally design synthetic molecules that can be optimized for inhibition of protein-protein interactions. Structural information on the HDM2-p53 complex was used to design our first class of peptoid inhibitors, and we provide here, in detail, the strategy to modify peptoids with the appropriate side chains that are effective inhibitors of HDM2-p53 binding. While we initially tried to develop rigid, helical peptoids as HDM2 binders, the best inhibitors were surprisingly peptoids that lacked any helix-promoting groups. These results indicate that starting with rigid peptoid scaffolds may not always be optimal to develop new inhibitors.
SuFExable Isocyanides for Ugi Reaction: Synthesis of Sulfonyl Fluoro Peptides
Xu, Shuheng,Cui, Sunliang
supporting information, p. 5197 - 5202 (2021/07/20)
Herein, the sulfonyl fluoro isocyanides were first developed as a new type of SuFExable synthon, and they are used as building blocks in the Ugi reaction (U-4CR). The Ugi reaction was established and the substrate scope was investigated, and various sulfonyl fluoro α-amino amides and peptides could be reached in a one-step synthesis. Therefore, this protocol opens a new vision for SuFExable building blocks and click chemistry, and it also provides a distinct approach to sulfonyl fluoro peptides.
PROCESS FOR THE PREPARATION OF TAUROLIDINE AND ITS INTERMEDIATES THEREOF
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Paragraph 0025, (2013/09/26)
The present invention relates to a process for the preparation of substantially pure Taurolidine.
4-(SUBSTITUTED ANILINO)QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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Page/Page column 14, (2012/08/14)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositons and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
4-(Substituted Anilino)-Quinazoline Derivatives Useful as Tyrosine Kinase Inhibitors
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Page/Page column 9, (2012/08/28)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
PROCESS FOR THE PREPARATION OF TAUROLIDINE AND ITS INTERMEDIATES THEREOF
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Page/Page column 3-4, (2012/06/15)
The present invention relates to a process for the preparation of substantially pure Taurolidine.
A simple large-scale synthesis of Cbz-protected taurylsulfonyl azide
Brouwer, Arwin J.,Liskamp, Rob M. J.
experimental part, p. 2228 - 2230 (2011/11/12)
A simple and efficient method for the large-scale synthesis of Cbz-taurylsulfonyl azide is described. This sulfonyl azide is accessible from taurine using three or four synthetic steps. Georg Thieme Verlag Stuttgart - New York.
Synthesis of β-aminoethanesulfonyl fluorides or 2-substituted taurine sulfonyl fluorides as potential protease inhibitors
Brouwer, Arwin J.,Ceylan, Tarik,Linden, Tima van der,Liskamp, Rob M.J.
body text, p. 3391 - 3393 (2009/09/05)
Substituted taurine sulfonyl fluorides derived from taurine or protected amino acids are conveniently synthesized from β-aminoethanesulfonyl chlorides using KF/18-crown-6 or from β-aminoethanesulfonates using DAST.
NEW COMPOUNDS
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Page/Page column 52, (2008/06/13)
The present invention relates to new compounds of formula Ia or Ib wherein P represents a 5- or 6-membered heteroaromatic ring containing one or two heteroatoms selected independently from N, O and S of which at least one heteroatom is nitrogen; R is hydrogen; R is selected from: C1-6alkyl, cyano, halogen, (CO)OR, and CONRR; R is selected from: C1-6alkyl, cyano, nitro, (CO)OR, C1-6alkylNRR, OC2-6alkylNRR, CONRR, and (SO2)NRR; m is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; as a free base or a salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
