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

DOI: 10.1021/jm201454n

Source and publish data:

Journal of Medicinal Chemistry p. 2623 - 2640 (2012)

Update date:2022-08-05

Topics:

Authors:

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.

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Article abstract of DOI:10.1021/jm201454n

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 (

Full text of DOI:10.1021/jm201454n

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