Asymmetric Synthesis of Norcantharidin Analogues by Alkynylation of Oxabenzonorbornadienes and Their Anticancer Activities
The present invention relates to chemical entities originated from natural sources or obtained from a chemically synthesized compound and further synthesized for therapeutic uses. More particularly, the present invention relates to norcantharidin analogues synthesized by a transition metal-catalyzed alkynylation of oxanorbornadiene derivatives and their antitumor effects.
Reducing the side-effect in the urinary system to some extent and increasing the number of white blood cells with comparable anti-cancer activity
Used as an anticancer agent in clinical application
The norcantharidin analogues of the present invention are originated from natural sources and further synthesized into at least three different compounds. using an Ir catalyst to carry out transition metal-catalyzed alkynylation of oxanorbornadiene derivatives.
Inventor: Chan, Albert Sun-Chi | Fan, Baomin | Wang, Jun | Lin, Chengyuan | Huang, Chao | Yang, Qingjing | Xu, Jianbin | Bian, Zhaoxiang | Lu, Aiping | Hu, Jun
Priority Number: US8835658B2
IPC Current: C07D030700 | C07D049308
US Class: 549459
Assignee Applicant: Hong Kong Baptist University
Title: Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities
Usefulness: Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities
Summary: (I) is useful for treating cancer tumors including colorectal carcinoma and breast adenocarcinoma (all claimed). Test details are described but no results given.
Novelty: Synthesizing norcantharidin compounds, useful for treating cancer tumors e.g. colorectal carcinoma, comprises alkynylation of oxabenzonorbornadienes in presence of catalyst including transition metal compound and biaryl diphosphine ligand
Disease Diagnostic/Treatment
Cancer/Tumor
2012.12.28
US 13/729,479
Filed
G06/CY/Lipp/US01
Hong Kong
