71759-92-7Relevant articles and documents
Synthesis, Structure and Antitumoural Activity of Triazole-Functionalised NHC–Metal Complexes
Monticelli, Marco,Bellemin-Laponnaz, Stéphane,Tubaro, Cristina,Rancan, Marzio
, p. 2488 - 2495 (2017)
Silver(I), gold(I), copper(I) and ruthenium(II) N-heterocyclic carbene (NHC) complexes have been synthesised and their cytotoxic activities towards various cancer cell lines have been evaluated. The N-heterocyclic carbene ligand has been functionalised with a 1,2,3-triazole moiety tethered in the backbone of the ligand. The molecular structure of the silver(I) and gold(I) complexes has been solved by X-ray diffraction analysis. The AgI, AuI and RuII complexes display good stability in aqueous conditions and show cytotoxic activities comparable or slightly superior to those of similar unfunctionalised complexes.
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant
Thomas, Mathew,Huang, Wei-Sheng,Wen, David,Zhu, Xiaotian,Wang, Yihan,Metcalf, Chester A.,Liu, Shuangying,Chen, Ingrid,Romero, Jan,Zou, Dong,Sundaramoorthi, Raji,Li, Feng,Qi, Jiwei,Cai, Lisi,Zhou, Tianjun,Commodore, Lois,Xu, Qihong,Keats, Jeff,Wang, Frank,Wardwell, Scott,Ning, Yaoyu,Snodgrass, Joseph T.,Broudy, Marc I.,Russian, Karin,Iuliucci, John,Rivera, Victor M.,Sawyer, Tomi K.,Dalgarno, David C.,Clackson, Tim,Shakespeare, William C.
scheme or table, p. 3743 - 3748 (2011/08/06)
Ponatinib (AP24534) was previously identified as a pan-BCR-ABL inhibitor that potently inhibits the T315I gatekeeper mutant, and has advanced into clinical development for the treatment of refractory or resistant CML. In this study, we explored a novel series of five and six membered monocycles as alternate hinge-binding templates to replace the 6,5-fused imidazopyridazine core of ponatinib. Like ponatinib, these monocycles are tethered to pendant toluanilides via an ethynyl linker. Several compounds in this series displayed excellent in vitro potency against both native BCR-ABL and the T315I mutant. Notably, a subset of inhibitors exhibited desirable PK and were orally active in a mouse model of T315I-driven CML.
Terminal alkynes from aldehydes via dehydrohalogenation of (Z)-1-iodo-1-alkenes with TBAF
Beshai, Mira,Dhudshia, Bhartesh,Mills, Ryan,Thadani, Avinash N.
supporting information; experimental part, p. 6794 - 6796 (2009/04/07)
Terminal alkynes were prepared in near quantitative yields via dehydrohalogenation of (Z)-1-iodo-1-alkenes with tetrabutylammonium fluoride (TBAF) under mild conditions. The methodology was expanded to include a one-pot, direct synthesis of terminal alkynes from aldehydes without the necessity of isolating and purifying the intermediate iodoalkene.
