TRICYCLIC DITERPENE ANALOGUE, AND SYNTHESIS AND APPLICATION THEREOF

WIPO Patent Application WO/2023/030043

A1

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.

QIU WENWEI (CN)
SONG BAOLIANG (CN)
HE LIMING (CN)
LIU YUANBIN (CN)

PCT/CN2022/113625

March 09, 2023

August 19, 2022

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CHOLESGEN SHANGHAI CO LTD (CN)

C07C235/78; A61K31/16; A61P35/00; C07C51/16; C07C53/132; C07C231/02

CN104557602A	2015-04-29
CN106928147A	2017-07-07
US20030232786A1	2003-12-18
CN113244249A	2021-08-13
TW201613574A	2016-04-16
CN101066916A	2007-11-07

MSJLAW OFFICE (CN)

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