Targeted indoleamine-2,3-dioxygenase 1 nitrogen mustard inhibitor as well as preparation method and application thereof

A compound and amino technology, applied in the field of medicine, can solve the problems of unreported research on multi-target inhibitors, achieve good IDO1 inhibitory activity, delay tumor growth, and broad-spectrum anti-tumor activity in vitro
CN107987031AInactive Publication Date: 2018-05-04EAST CHINA UNIV OF SCI & TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
EAST CHINA UNIV OF SCI & TECH
Publication Date
2018-05-04
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a targeted indoleamine-2,3-dioxygenase 1 nitrogen mustard inhibitor as well as a preparation method and application thereof. A structure of the inhibitor is shown as a generalformula I, wherein definition of R is as shown in the claims and specification. Pharmacological experiments prove that the compound disclosed by the invention has excellent IDO1 inhibitory activity and has broad-spectrum in-vitro antitumor activity. In-vivo experiments prove that the compound disclosed by the invention can achieve effects of down-regulating the in-vivo IDO1 activity and obviouslydelaying tumor growth, and can be applied to preparing IDO1-mediated medicines for tumor diseases with pathological features in a tryptophan metabolism pathway. The structural formula is as shown in the specification.
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Description

technical field

[0001] The invention relates to the technical field of medicine, in particular to a nitrogen mustard inhibitor targeting indoleamine-2,3-dioxygenase 1 and its preparation method and application. Background technique

[0002] Nitrogen mustards are still an important class of antineoplastic drugs in clinical application, such as Chlorambucil and Melphalan.

[0003]

[0004] The mechanism of action of this type of antitumor drug is that it can form electron-deficient ethyleneimine ions in the body, and then co-exist with electron-rich groups in biomacromolecules (such as DNA, RNA, or some important enzymes). Valence binding, inactivation or DNA molecule breakage, so as to achieve anti-tumor effect. Nitrogen mustard drugs have the advantages of broad anti-tumor spectrum and strong lethality to tumor cells, but they also have disadvantages such as low therapeutic efficiency, poor selectivity, and large toxic and side effects.

[0005] Indoleamine 2,3-dioxygen...

Claims

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