57121-48-9Relevant academic research and scientific papers
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.
Synthesis and biological evaluation of 1-[2-cyano-3,12-dioxooleana-1,9(11)- dien-28-oyl]-4-ethynylimidazole. A novel and highly potent anti-inflammatory and cytoprotective agent
Honda, Tadashi,Dinkova-Kostova, Albena T.,David, Emilie,Padegimas, Eric M.,Sundararajan, Chitra,Visnick, Melean,Bumeister, Ron,Christian Wigley
scheme or table, p. 2188 - 2191 (2011/06/17)
To explore more potent N-acylimidazole analogues of CDDO than CDDO-Im, which is one of the most potent compounds in several widely used bioassays related to protection against inflammation and carcinogenesis; we have synthesized and evaluated five new N-a
A stereospecific route to (Z)-Urocanic acids
Despinoy, Xavier L. M.,McNab, Hamish,Tyas, Richard G.
, p. 1676 - 1678 (2008/12/22)
(Z)-Urocanic acid and its derivatives can be made stereo-specifically by ring-opening of pyrrolo[l,2-c]imidazol-5-ones in aqueous tetrahydrofuran.
1H-4(5)-substituted imidazole derivatives
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, (2008/06/13)
The present invention provides, in its principal aspect, compounds of the general formula: when A is -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=CH-, -COCH2-, CH2CH2-, -CH(OH)CH2- or -C 3BOND C-; X can be H, CH3, NH2, NH(CH3),N(CH3)2, OH, OCH3, SH, R2
