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Synthesis and Biological Evaluation of Oxindole Sulfonamide Derivatives as Bruton's Tyrosine Kinase Inhibitors**
ChemMedChem ( IF 3.6 ) Pub Date : 2023-11-02 , DOI: 10.1002/cmdc.202300511
Chandra Prakash Koraboina 1 , Venkatanarayana Chowdary Maddipati 1 , Narendran Annadurai 2 , Soňa Gurská 2, 3 , Petr Džubák 2, 3 , Marián Hajdúch 2, 3 , Viswanath Das 2, 3 , Rambabu Gundla 1
Affiliation  

A series of 3-(dihydro-2H-pyran-4(3H)-ylidene)-2-oxoindoline-5-sulfonamide derivatives were synthesized by Knoevenagel condensation of dihydro-2H-pyran-4(3H)-one in the presence of pyrrolidine with corresponding sulfonamides. The new oxindole sulfonamide PID-4 selectively inhibited BTK-high RAMOS cell proliferation and phosphorylation of BTK and downstream signalling cascades.

中文翻译:

作为布鲁顿氏酪氨酸激酶抑制剂的羟吲哚磺酰胺衍生物的合成和生物学评价**

以二氢-2H-吡喃-4(3H ) -亚基)-2-氧代吲哚啉-5-磺酰胺为原料,通过Knoevenagel缩合反应合成了一系列3-(二氢-2H-吡喃-4( 3H )-亚基)-2-氧代吲哚啉-5-磺酰胺衍生物在吡咯烷和相应的磺酰胺存在下。新型羟吲哚磺酰胺PID-4选择性抑制 BTK 高 RAMOS 细胞增殖以及 BTK 和下游信号级联的磷酸化。
更新日期:2023-11-02
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