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filingDate 2021-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4a7cb8294ccf73343d100c2d36e71277
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publicationDate 2022-12-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber KR-20220162364-A
titleOfInvention Novel squaramide derivatives and use thereof
abstract The present invention relates to a novel square amide derivative and its use, and provides a novel derivative that exhibits anticancer activity through eIF2α phosphorylation by using a strategy of substituting a urea parent compound with a bioisostere, square amide. Square amides contain a specific structure with a double bond linked to a carbonyl group. A square amide structure can be created by mediating a precursor having an amine group on a squarate ring of a square ring through a conjugate addition reaction. The present invention efficiently constructs a key intermediate in which an aniline ring with various substituents is introduced into a square amide, and utilizes this to provide a derivative in which a phenoxycyclohexyl structure is introduced to the opposite nitrogen. Since the synthesized novel derivative shows eIF2α phosphorylation effect and cancer cell proliferation inhibitory activity in vitro, it can be used as an anticancer agent.
priorityDate 2021-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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