Wu, Guolin published the artcileSynthesis and structure-activity relationship studies of MI-2 analogues as MALT1 inhibitors, Name: 2-Morpholinoethanol, the publication is Bioorganic & Medicinal Chemistry (2018), 26(12), 3321-3344, database is CAplus and MEDLINE.
Recent studies revealed that MALT1 is a promising therapeutic target for the treatment of ABC-DLBCL. Among several reported MALT1 inhibitors, MI-2 as an irreversible inhibitor represents a new class of ABC-DLBCL therapeutics. Due to its inherent potential cross-reactivity, further structure-activity relationship (SAR) study is imperative. Five focused compound libraries based on the chem. structure of MI-2 are designed and synthesized. The systematic SARs revealed that the side chain of 2-methoxyethoxy has little impact on the activity and can be replaced by other functionalized groups, providing new MI-2 analogs with retained or enhanced potency. Compounds 81-83 with terminal hydroxyl group as side chain displayed enhanced activities against MALT1. Replacement of triazole core with pyrazole is also tolerant, while structural modifications on other sites are detrimental. These findings will facilitate further development of small-mol. MALT1 inhibitors.
Bioorganic & Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C15H16O3, Name: 2-Morpholinoethanol.
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