Xn:Harmful;16694-18-1Relevant articles and documents
COMPOSITIONS AND METHODS OF TARGETING MUTANT K-RAS
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Paragraph 0397; 0398, (2018/08/03)
Compounds and compositions are presented that inhibit K-Ras, and especially mutant K-Ras. Certain compounds preferentially or even selectively inhibit specific forms of mutant K-Ras, and particularly the G12D mutant form.
Direct bromination of ethyl 5-alkylthiophene-2-carboxylates
Taydakov, Ilya V.,Krasnoselskiy, Sergey S.
body text, p. 2965 - 2968 (2010/10/19)
Approaches to brominated thiophene-2-carboxylic acids by electrophilic bromination of the corresponding acids and esters were compared and investigated. A synthetic route was developed involving direct bromination of ethyl 5-alkylthiophene-2-carboxylates followed by saponification of the resulting ethyl 5-alkyl-4-bromothiophene-2-carboxylates. The key bromination step is selective in dichloromethane solution at 0-5 °C and furnishes the corresponding ethyl 5-alkyl-4-bromothiophene-2-carboxylates in excellent yields. No migration or isomerization of the alkyl substituents was observed. Georg Thieme Verlag Stuttgart New York.
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors
Dublanchet, Anne-Claude,Ducrot, Pierre,Andrianjara, Charles,O'Gara, Margaret,Morales, Renaud,Compere, Delphine,Denis, Alexis,Blais, Stephane,Cluzeau, Philippe,Courte, Karine,Hamon, Jacques,Moreau, Francois,Prunet, Marie-Laure,Tertre, Anita
, p. 3787 - 3790 (2007/10/03)
A new class of MMP-12 inhibitors was discovered and optimized using structure-based drug design methods. Modeling studies using a known MMP-12 crystal structure identified a new interaction mode for these new MMP-12 inhibitors. Further optimization resulted in the discovery of a compound displaying nanomolar activity against MMP-12 and which was co-crystallized with MMP-12.
