Analogue of Nanocystin A as well as preparation method and application of analogue

A technology of analogues and compounds, applied in the field of analogues of NannocystinA and its preparation, can solve the problems of limited natural product sources and difficulty in obtaining sufficient quantities of compounds, and achieve the effects of simple structure, short synthetic route and high target yield
CN112321677AInactive Publication Date: 2021-02-05PEKING UNIV SHENZHEN GRADUATE SCHOOL +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
PEKING UNIV SHENZHEN GRADUATE SCHOOL
Publication Date
2021-02-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an analogue of Nannocystin A as well as a preparation method and application of the analogue. The analogue of the Nanocystin A has a molecular structural formula as shown in ageneral formula I in the specification, wherein R in the general formula I is arbitrary one of -H, C1-C15 alkyl, aryl, C1-C15 alkoxy, halogen, hydroxyl, amino, nitro, cyano and sulfydryl. The analogueof Nannocystin A has a simple structure, has a biological effect of inhibiting the activity of cancer cells, and can optimize the biological activity of Nannocystin A by regulating the variety of R contained in Nannocystin A. The analogue of the Nannocystin A further confirms the structure-activity relationship, and lays an excellent foundation for searching compounds with better anti-cancer activities. The preparation method has a short synthesis circuit, high target yield and few byproducts.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis and medicinal chemistry, and in particular relates to an analog of Nannocystin A and its preparation method and application. Background technique

[0002] In 2015, Mark Bronstrup (Holger Hoffmann, et al. Angew. Chem. Int. Ed. 2015, 54, 10145-10148) and others isolated a macrocyclic lipopeptide compound Nannocystin from myxobacterial genus, Nannocystis sp. A, The molecule has a novel 21-membered ring backbone containing a tripeptide and a polyketide segment with epoxyamide. In September 2016, our research group (Tao Ye, etal. Angew. Chem. Int. Ed. 2016, 55, 13263–13266) completed the first total synthesis of this molecule.

[0003] In terms of biological activity testing, the article shows that Nannocystin A not only has strong antibacterial activity, but also inhibits cell proliferation by inducing apoptosis at the nanomolar level. In July of the same year, Dominic Hoepfner (PhilippKra...

Claims

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