Homocamptothecin norcantharidinate derivative, and regioselective synthesis method thereof
A cantharidinate and regioselective technology, which can be applied in the fields of drug combination, organic chemistry, antitumor drugs, etc., can solve the problems of high toxicity and low bioavailability of camptothecin, and achieve easy availability of raw materials and low cost. , Good anti-cancer effect
Active Publication Date: 2019-11-12
甘肃松盛医药有限公司
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Problems solved by technology
Researchers such as VIshnuvajjala and Garzon-Aburbeh have successively reported the high toxicity and low bioavailability of camptothecin in vivo, so they cannot be directly used as anticancer clinical reagents
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[0023] The following will further illustrate the present invention through specific examples, but it is not intended to limit the protection scope of the present invention. Without departing from the concept of the present invention, those skilled in the art may make improvements or combinations to the parameters or conditions of the claims, and these improvements or combinations shall also be regarded as the protection scope of the present invention. Therefore, the protection scope of the patent for the present invention should be based on the appended claims. The solvents and reagents used in the present invention come from Sinopharm Group Shanghai Reagent Company. Unless otherwise specified, all reagents used were chemically pure.
[0024] Synthetic General Method for Preparation of Synthetic Compound II by Prior Art and Literature
[0025]
[0026] R is selected from C 1 -C 6 Alkyl, benzyl, substituted benzyl
[0027] Referring to the literature, the reaction of f...
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The invention provides a homocamptothecin norcantharidinate derivative I and a regioselective synthesis method thereof in the fields of design and synthesis of novel drugs. The homocamptothecin norcantharidinate derivative I has a structural formula as shown in a formula I which is described in the specification. In the formula I, R is selected from the group consisting of C1-C6 alkyl, substitutedalkyl and cycloalkyl groups. Activity test results prove that the homocamptothecin norcantharidinate derivative I designed and synthesized by using the method provided by the invention has good antitumor effect, and specifically has high activity on liver cancer, gastric cancer, colon cancer and pancreatic cancer. In addition, the method for preparing the homocamptothecin norcantharidinate derivative I provided by the invention has the advantages of easily-available raw materials, low cost, extremely-high synthesis reaction regioselectivity and high target product yield; and the homocamptothecin norcantharidinate derivative I provided by the invention is easy to be prepared.
Description
technical field [0001] The invention belongs to the field of new drug design and synthesis, and in particular relates to a novel homocamptothecin norcantharidin ester derivative and its regioselective synthesis method and anti-tumor application. Background technique [0002] TopoIsomerase I is an important DNA regulatory enzyme. Several research groups such as Staker have confirmed that this enzyme is the only target of camptothecin to exert anti-tumor activity, and its pharmacological mechanism is linked to the interface of covalent protein-nucleic acid conjugates. Camptothecin was first discovered in the bark extract of Camptotheca acumInate by the WanI research group of NCI in the early 1960s. Researchers such as VIshnuvajjala and Garzon-Aburbeh have successively reported the high toxicity and low bioavailability of camptothecin in the body, so it cannot be directly used as an anticancer clinical reagent. [0003] Studies have shown that the quinoline ring of CPT can be ...
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IPC IPC(8): C07D519/00A61P35/00
CPCC07D519/00A61P35/00
Inventor 赵长阔王先恒袁智
Owner 甘肃松盛医药有限公司