Makowski, Kamil published the artcileSudemycin K: A Synthetic Antitumor Splicing Inhibitor Variant with Improved Activity and Versatile Chemistry, SDS of cas: 945953-41-3, the publication is ACS Chemical Biology (2017), 12(1), 163-173, database is CAplus and MEDLINE.
Important links exist between the process of pre-mRNA splicing and cancer, as illustrated by the frequent mutation of splicing factors in tumors and the emergence of various families of anti-tumor drugs that target components of the splicing machinery, notably SF3B1, a protein subunit of spliceosomal U2 small nuclear Ribonucleoprotein Particle (snRNP). Sudemycins are synthetic compounds that harbor a pharmacophore common to various classes of splicing inhibitors. Here we describe the synthesis and functional characterization of novel Sudemycin analogs that functionally probe key functional groups within this pharmacophore. Our results confirm the importance of a conjugated diene group and in addition reveal significant spatial flexibility in this region of the mol. Sudemycin K, a derivative that replaces the pharmacophore oxycarbonyl by an amide group, displays improved potency as an inhibitor of cancer cell proliferation, as a regulator of alternative splicing in cultured cells and as an inhibitor of in vitro spliceosome assembly. Sudemycin K displays higher stability, likely related to the replacement of the oxycarbonyl group, which can be substrate of esterases, by an amide group. The activity and special reactivity of Sudemycin K can pave the way to the synthesis and evaluation of a variety of novel Sudemycin derivatives
ACS Chemical Biology published new progress about 945953-41-3. 945953-41-3 belongs to piperazines, auxiliary class Piperazine,Amide,Aldehyde, name is tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate, and the molecular formula is C11H20N2O3, SDS of cas: 945953-41-3.
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https://en.wikipedia.org/wiki/Piperazine,
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