916791-10-1Relevant articles and documents
Discovery of the macrocycle (9 E)-15-(2-(Pyrrolidin-1-yl)ethoxy)-7,12,25- trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9, 14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of Janus kinase 2/Fms-liketyrosine kinase-3 (J
William, Anthony D.,Lee, Angeline C.-H.,Poulsen, Anders,Goh, Kee Chuan,Madan, Babita,Hart, Stefan,Tan, Evelyn,Wang, Haishan,Nagaraj, Harish,Chen, Dizhong,Lee, Chai Ping,Sun, Eric T.,Jayaraman, Ramesh,Pasha, Mohammad Khalid,Ethirajulu, Kantharaj,Wood, Jeanette M.,Dymock, Brian W.
experimental part, p. 2623 - 2640 (2012/06/01)
Herein, we describe the synthesis and SAR of a series of small molecule macrocycles that selectively inhibit JAK2 kinase within the JAK family and FLT3 kinase. Following a multiparameter optimization of a key aryl ring of the previously described SB1518 (