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Nitric oxide donor-type farnesyl thiosalicylic acid derivative, and preparation method and medical application thereof

A technology of farnesyl thiosalicylic acid and its derivatives, applied in the field of application in the preparation of antitumor drugs

Inactive Publication Date: 2010-08-25
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The present invention discloses a class of furazan nitrogen oxide NO-donor FTA derivatives with medicinal value and pharmaceutically acceptable salts thereof. There is no report on this type of compound so far

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  • Nitric oxide donor-type farnesyl thiosalicylic acid derivative, and preparation method and medical application thereof
  • Nitric oxide donor-type farnesyl thiosalicylic acid derivative, and preparation method and medical application thereof
  • Nitric oxide donor-type farnesyl thiosalicylic acid derivative, and preparation method and medical application thereof

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Abstract

The invention discloses a nitric oxide (NO) donor-type farnesyl thiosalicylic acid (FTA) derivative, and pharmaceutically acceptable salt, a preparation method and medical application thereof. The FTA derivative is a compound obtained by carrying out heterozygosis on a NO donor furazan nitrogen oxide and Ras protein inhibitor FTA by an ester bond or an amido bond. Pharmacological test results show that the FTA derivative can reserve the Ras protein inhibiting activity of FTA and simultaneously releases high-concertration NO to induce cancer cell apoptosis and enhance the inhibiting action on cancer cell proliferation; compared with the FTA, the FTA derivative has more excellent anti-tumor activity, and therefore, the compound can be suitable for treating various clinical malignant tumours.

Description

technical field The present invention relates to the field of medicine, in particular to a class of nitric oxide donor type farnesyl thiosalicylic acid derivatives and pharmaceutically acceptable salts thereof, their preparation methods, pharmaceutical compositions containing these derivatives and their The medical application, especially the application in the preparation of antineoplastic drugs. Background technique All-trans farnesylthiosalicylic acid (abbreviation: FTA, trade name: Salirasib), as a new farnesyltransferase-based Ras protein inhibitor, can competitively replace F-Ras and F-Ras mutant proteins with Galectin binds and inhibits Ras-induced downstream signaling pathways (including Raf and P13K signaling pathways) and mTOR (stimulator of tumorigenesis, which can rely on or independently open P13K signaling pathways), thereby inhibiting the growth of tumor cells. Studies have shown that FTA can inhibit cell proliferation and migration of various tumors (glioma,...

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Application Information

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IPC IPC(8): C07D413/12C07D271/08A61K31/625A61P35/00A61P35/02
Inventor 张奕华凌勇赖宜生叶小磊季晖彭司勋
Owner CHINA PHARM UNIV
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