Title:
NAPHTHYL UREA COMPOUND HAVING ANTI-CANCER EFFECT, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/214106
Kind Code:
A1
Abstract:
Disclosed are a naphthyl urea compound having anti-cancer effect, a preparation method therefor, and a use thereof. The naphthalene urea parent nucleus radical group contained therein having biological activity is further chemically modified to generate compound groups having higher biological activity, expanding the wide biomedical application and pharmaceutical development prospects of the present compound. The present compound can substantially inhibit the activation of JAK2/STAT3 signal at a low dosage (submicromolar). The MTT, molecular docking, and western blotting experiment results show that the compound can specifically inhibit the activation of JAK2 signal and the expression of target genes such as downstream STAT3, cyclin D1, cyclin B1, and MMP9, induce cell cycle block and apoptosis, and substantially inhibit the proliferation of multiple tumor cell strains such as breast cancer, liver cancer, lung cancer, drug resistant lung cancer, colon cancer, and leukemia, highlighting the prospect of the present compound in the development as JAKs/STAT3 targeted anti-cancer medications.
Inventors:
XU MARVIN XUEJUN (CN)
YANG YUPO (CN)
YANG ZHENGYAN (CN)
XU HONGYUN (CN)
DUAN CHAOQUN (CN)
DONG JIAWEI (CN)
YANG YUPO (CN)
YANG ZHENGYAN (CN)
XU HONGYUN (CN)
DUAN CHAOQUN (CN)
DONG JIAWEI (CN)
Application Number:
PCT/CN2022/092155
Publication Date:
October 13, 2022
Filing Date:
May 11, 2022
Export Citation:
Assignee:
HENAN RADIOMEDICAL SCIENCE AND TECH CO LTD (CN)
International Classes:
C07D401/12; A61K31/4453; A61K31/4525; A61K31/453; A61K31/4545; A61P35/00; A61P35/02; C07D211/06; C07D405/12
Foreign References:
| CN113444035A | 2021-09-28 | |||
| CN112961120A | 2021-06-15 | |||
| CN110526881A | 2019-12-03 | |||
| CN111559991A | 2020-08-21 | |||
| CN114702439A | 2022-07-05 |
Attorney, Agent or Firm:
ZHENGZHOU LIANKE PATENT AGENCY (COMMON PARTNERSHIP) (CN)
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