1168106-39-5Relevant articles and documents
Eucalyptol as bio-based solvent for Migita–Kosugi–Stille coupling reaction on O,S,N-heterocycle
Campos, Joana F.,Berteina-Raboin, Sabine
, p. 138 - 142 (2020)
We report herein an investigation on the use of eucalyptol as new solvent for organic transformations applied to the Migita-Kosugi-Stille palladium-catalyzed cross-coupling reaction. Heterocycles containing oxygen, sulfur and nitrogen were chosen as starting materials. Eucalyptol turned out to be a viable sustainable alternative to common solvents for this reaction.
Synthesis and biological evaluation of selected 7H-pyrrolo[2,3-d]pyrimidine derivatives as novel CDK9/CyclinT and Haspin inhibitors
Baratte, Blandine,Beteck, Richard M.,Jesumoroti, Omobolanle J.,Legoabe, Lesetja J.,Pieterse, Lianie,Robert, Thomas,Ruchaud, Sandrine,Bach, Stéphane
, (2021/09/20)
Protein kinases, including CDK9/CyclinT and Haspin, are regarded as potential drug targets in cancer therapy. Findings from a previous study suggested 7-azaindole as a privileged scaffold for producing inhibitors of CDK9/CyclinT and Haspin. Inspired by these findings, the current study synthesised and evaluated thirteen (13) C6-substituted 7-azaindole and twenty (20) C4-substituted structurally related 7H-pyrrolo[2,3-d]pyrimidine derivatives against a panel of protein kinases, including CDK9/CyclinT and Haspin. Eleven of the 7H-pyrrolo[2,3-d]pyrimidine derivatives exhibited activity toward CDK9/CyclinT, while 4 of compounds had activity against Haspin. The best CDK9/CyclinT (IC50 of 0.38 μM) and Haspin (IC50 of 0.11 μM) activities were achieved by compounds 7d and 7f, respectively. Hence, these compounds may be valuable starting points for development of new anti-cancer drugs.
NOVEL 6-SUBSTITUTED 7-DEAZAPURINES AND CORRESPONDING NUCLEOSIDES AS MEDICAMENTS
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Page/Page column 25-26; 47; 51; 52, (2021/08/27)
The present invention relates to the synthesis of 6-substituted 7-deazapurines and their corresponding nucleosides by coupling aryl or alkyl Grignard reagents with halogenated purine nucleosides in the presence of iron or an iron/copper mixture such as Fe(acac)3/Cul. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections.