668970-91-0Relevant academic research and scientific papers
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
Keeley,ábrányi-Balogh,Keseru
, p. 263 - 267 (2019/03/05)
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed correlations between the electronic properties of the heterocyclic cores and their reactivity against GSH that are helpful in identifying suitable fragments for cysteines with specific nucleophilicity. The most important advantage of these fragments is that they show only minimal structural differences from non-electrophilic counterparts. Therefore, they could be used effectively in the design of targeted covalent inhibitors with minimal influence on key non-covalent interactions.
GOLD (I)-PHOSPHINE 1,2,3-TRIAZOLE DERIVATIVES WITH ANTIOBIOTIC PROPERTIES
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, (2020/01/11)
The present invention relates to gold (l)-phosphine 1,2,3-triazole compounds, and their use in a human or animal medicine. The present invention also relates to using such compounds for the prevention and/or treatment of an infection, i.e. inhibitors of growth of Gram-positive and/or Gram-negative bacteria. On another aspect the invention relates to the synthesis of the gold (l)-phosphine compounds of the invention and to their synthesis intermediates. The present invention finds applications in the medical, veterinary and/or chemical fields.
Structure-based design of orally bioavailable 1 h -Pyrrolo[3,2- C ]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)
Naud, Sébastien,Westwood, Isaac M.,Faisal, Amir,Sheldrake, Peter,Bavetsias, Vassilios,Atrash, Butrus,Cheung, Kwai-Ming J.,Liu, Manjuan,Hayes, Angela,Schmitt, Jessica,Wood, Amy,Choi, Vanessa,Boxall, Kathy,Mak, Grace,Gurden, Mark,Valenti, Melanie,De Haven Brandon, Alexis,Henley, Alan,Baker, Ross,McAndrew, Craig,Matijssen, Berry,Burke, Rosemary,Hoelder, Swen,Eccles, Suzanne A.,Raynaud, Florence I.,Linardopoulos, Spiros,Van Montfort, Rob L. M.,Blagg, Julian
, p. 10045 - 10065 (2014/01/17)
The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 genes overexpressed in tumors with chromosomal instability and aneuploidy. PTEN-defic
7-AZAINDOLE INHIBITORS OF CRAC
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, (2013/06/28)
Disclosed are compounds of Formula (I), useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
ANTIBACTERIAL BENZOIC ACID DERIVATIVES
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Page 288, (2010/02/06)
The invention provides antimicrobial agents and methods of using the agents for sterilization, sanitation, antisepsis, disinfection, and treatment of infections in mammals.
