Multiplexed Thiol Reactivity Profiling for Target Discovery of Electrophilic Natural Products.
Sign Up to like & getrecommendations! Published in 2017 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2017.08.022
Abstract: Electrophilic groups, such as Michael acceptors, expoxides, are common motifs in natural products (NPs). Electrophilic NPs can act through covalent modification of cysteinyl thiols on functional proteins, and exhibit potent cytotoxicity and anti-inflammatory/cancer activities. Here… read more here.
Keywords: reactivity profiling; target; discovery; reactivity ... See more keywords
Masking thiol reactivity with thioamide, thiourea, and thiocarbamate-based MBPs.
Sign Up to like & getrecommendations! Published in 2023 at "Chemical communications"
DOI: 10.1039/d2cc06596g
Abstract: Thioamides, thioureas, and thiocarbamates are introduced as stable, sulfur-based metal-binding pharmacophores (MBPs) for use in metalloenzyme fragment-based drug discovery (mFBDD). MBP reactivity, bioactivity, and structural studies show that these molecules can act as ligands for… read more here.
Keywords: thiourea thiocarbamate; thiol reactivity; thioamide thiourea; masking thiol ... See more keywords
(E)-2-Benzylidenecyclanones: Part XX—Reaction of Cyclic Chalcone Analogs with Cellular Thiols: Unexpected Increased Reactivity of 4-Chromanone- Compared to 1-Tetralone Analogs in Thia-Michael Reactions
Sign Up to like & getrecommendations! Published in 2024 at "Molecules"
DOI: 10.3390/molecules29235493
Abstract: In vitro relative cytotoxicity (IC50 (IIb)/IC50 (IIIb) of (E)-3-(4′-methylbenzylidene)-4-chromanone (IIIb) towards human Molt 4/C8 and CEM T-lymphocytes showed a >50-fold increase in comparison to those of the respective tetralone derivative (IIb). On the other hand,… read more here.
Keywords: part reaction; chromanone; thiol reactivity; reaction cyclic ... See more keywords