Title:
TRICYCLIC DITERPENE ANALOGUE, AND SYNTHESIS AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/030043
Kind Code:
A1
Abstract:
Disclosed are a tricyclic diterpene analogue represented by formula (I) and a preparation method therefor. By using testosterone as a raw material, and by means of methylation, ethylene glycol protection, oxidation, Baeyer-Villiger oxidation, reduction, hydrolysis and other reactions, and passing through cyanation and a Wittig reaction to extend a carbon chain, a corresponding parent nucleus compound is obtained; and the parent core compound is subjected to amidation to obtain the tricyclic diterpene analogue. Also disclosed is an application of the tricyclic diterpene analog in inhibiting a smoothened (SMO) protein and resisting against tumors. The tricyclic diterpene analog binds to a cysteine rich domain (CRD) at an N-terminal of the SMO protein to inhibit the activity of a hedgehog (Hh) signaling pathway, which thus inhibits the growth of tumor cells and has good tumor-resisting application prospects. In addition, the present application may solve the problem of drug resistance of existing clinical SMO inhibitors, thus providing a new solution for the treatment of related diseases.
Inventors:
QIU WENWEI (CN)
SONG BAOLIANG (CN)
HE LIMING (CN)
LIU YUANBIN (CN)
SONG BAOLIANG (CN)
HE LIMING (CN)
LIU YUANBIN (CN)
Application Number:
PCT/CN2022/113625
Publication Date:
March 09, 2023
Filing Date:
August 19, 2022
Export Citation:
Assignee:
CHOLESGEN SHANGHAI CO LTD (CN)
International Classes:
C07C235/78; A61K31/16; A61P35/00; C07C51/16; C07C53/132; C07C231/02
Foreign References:
CN104557602A | 2015-04-29 | |||
CN106928147A | 2017-07-07 | |||
US20030232786A1 | 2003-12-18 | |||
CN113244249A | 2021-08-13 | |||
TW201613574A | 2016-04-16 | |||
CN101066916A | 2007-11-07 |
Attorney, Agent or Firm:
MSJLAW OFFICE (CN)
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