Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK)

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Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK)

Trani, Giancarlo; Barker, John J; Bromidge, Steven M; Brookfield, Frederick A; Burch, Jason D; Chen, Yuan; Eigenbrot, Charles; Heifetz, Alexander; Ismaili, M Hicham A; Johnson, Adam; Krülle, Thomas M; MacKinnon, Colin H; Maghames, Rosemary; McEwan, Paul A; Montalbetti, Christian A G N; Ortwine, Daniel F; Pérez-Fuertes, Yolanda; Vaidya, Darshan G; Wang, Xiaolu; Zarrin, Ali A; Pei, Zhonghua

Bioorganic & medicinal chemistry letters, 12/2014, Letnik: 24, Številka: 24

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Starting from benzylpyrimidine 2, molecular modeling and X-ray crystallography were used to design highly potent inhibitors of Interleukin-2 inducible T-cell kinase (ITK). Sulfonylpyridine 4i showed sub-nanomolar affinity against ITK, was selective versus Lck and its activity in the Jurkat cell-based assay was greatly improved over 2.

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Leto	Faktor vpliva		Izdaja		Kategorija		Razvrstitev
Leto	JCR	SNIP	JCR	SNIP	JCR	SNIP	JCR	SNIP

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