cas 936138-17-9, 3-IODO-6-METHOXY-1H-INDAZOLE | Articles data ｜lookchem

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936138-17-9

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Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome
Using a structure based design approach we have identified a series of indazole substituted pyrrolopyrazines, which are potent inhibitors of JAK3. Intramolecular electronic repulsion was used as a strategy to induce a strong conformational bias within the ligand. Compounds bearing this conformation participated in a favorable hydrophobic interaction with a cysteine residue in the JAK3 binding pocket, which imparted high selectivity versus the kinome and improved selectivity within the JAK family.
Lynch, Stephen M.,Devicente, Javier,Hermann, Johannes C.,Jaime-Figueroa, Saul,Jin, Sue,Kuglstatter, Andreas,Li, Hongju,Lovey, Allen,Menke, John,Niu, Linghao,Patel, Vaishali,Roy, Douglas,Soth, Michael,Steiner, Sandra,Tivitmahaisoon, Parcharee,Vu, Minh Diem,Yee, Calvin
p. 2793 - 2800
(2013/07/05)

Synthesis of 3-indazolecarboxylic esters and amides via Pd-catalyzed carbonylation of 3-iodoindazoles
A straightforward and effective procedure for the preparation of 1H-indazole-3-carboxylic acid esters and amides was developed. A series of functionalized 3-iodoindazoles were subjected to Pd-catalyzed carbonylations in the presence of methanol or amines,
Buchstaller, Hans-Peter,Wilkinson, Kai,Burek, Kasimir,Nisar, Yasmin
experimental part
p. 3089 - 3098
(2011/10/13)

More Articles about upstream products of 936138-17-9

3522-07-4
6-methoxy-1H-indazole

More Articles about downstream products of 936138-17-9

Chemical Properties

Boiling Point: 393.1 °C at 760 mmHg
Flash Point:191.5 °C
Density: 1.941 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2–8 °C
Vapor Pressure: 4.96E-06mmHg at 25°C
Refractive Index: 1.727
PSA: 37.91000
LogP: 2.17610

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