Title:
NOVEL SQUARAMIDE DERIVATIVE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/255770
Kind Code:
A1
Abstract:
The present invention relates to a novel squaramide derivative and a use thereof and provides a novel derivative through the strategy of replacing a compound having a urea core with the bioisolate squaramide, whereby the derivative exhibits an anticancer activity through eIF2α phosphorylation efficacy. Squaramide has a characteristic structure retaining a double bond linked to the carbonyl groups. The squaramide structure can be prepared by mediating a precursor bearing an amine group to the squarate ring, which is a squaric ring, through a conjugate addition reaction. In the present invention, a core intermediate in which an aniline ring having various substituents is introduced into squaramide is effectively constructed and is used to provide a derivative in which a phenoxycyclohexyl structure is introduced into the opposite nitrogen. The synthesized novel derivative exhibits an eIF2α phosphorylation effect and an inhibitory activity against cancer cell proliferation in vitro, and thus can be used as a metabolic anticancer agent.
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Inventors:
YUN HWAYOUNG (KR)
JEONG JEE-YEONG (KR)
KWAK JINSOOK (KR)
KIM MIN JUNG (KR)
KIM SOYEONG (KR)
JEONG JEE-YEONG (KR)
KWAK JINSOOK (KR)
KIM MIN JUNG (KR)
KIM SOYEONG (KR)
Application Number:
PCT/KR2022/007722
Publication Date:
December 08, 2022
Filing Date:
May 31, 2022
Export Citation:
Assignee:
NAT UNIV PUSAN IND UNIV COOP FOUND (KR)
KOSIN UNIV INDUSTRY ACADEMY COOPERATION (KR)
KOSIN UNIV INDUSTRY ACADEMY COOPERATION (KR)
International Classes:
C07C255/28; A61K31/136; A61K31/18; A61P35/00; C07C255/60; C07C311/41; C07C317/32
Domestic Patent References:
| WO2018035346A1 | 2018-02-22 | |||
| WO2002083624A1 | 2002-10-24 |
Foreign References:
| CN111362871A | 2020-07-03 | |||
| CN111892536A | 2020-11-06 |
Other References:
TREMBLAY SéBASTIEN; BOUTIN JOëL; PERREAULT MARTIN; CôTé MARIE-FRANCE; GOBEIL STéPHANE; C.-GAUDREAULT REN&: "Synthesis and evaluation of substituted phenyl cycloalkylureas and bioisosteres as IL-6 expression inhibitors", MEDICINAL CHEMISTRY RESEARCH, vol. 29, no. 8, 19 May 2020 (2020-05-19), US , pages 1424 - 1437, XP037182157, ISSN: 1054-2523, DOI: 10.1007/s00044-020-02557-w
Attorney, Agent or Firm:
TAEBAEK INTELLECTUAL PROPERTY LAW FIRM (KR)
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