Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 mg/kg showed no toxicity response during the 14-day continuous observation period, indicating the high safety of the compounds, and the compounds can be used to prepare medicaments for preventing and treating carcinomas such as liver cancer, lung cancer. In the general structural formula of LQC-Y, R represents steroid compounds such as cholic acid, deoxycholic acid, ursodeoxycholic acid, chenodeoxycholic acid, and hyodeoxycholic acid and so on; triterpenoid compounds such as oleanolic acid, ursolic acid, pachymic acid, glycyrrhetinic acid and glycosides thereof and so on; emodic acid, emodin and other mono-substituted or poly-substituted structures of anthraquinone parent nucleus; baicalein, baicalin and other flavonoid; shikimic acid, mono-substituted shikimic acid or poly-substituted shikimic acid; gardenia acid and other iridoid acid derivatives; paeonol, curcumin and structural derivatives thereof.

Beijing University of Chinese Medicine

3D MEDICINES, LTD.

Synthesis and use of anti-tumor drug LQC-Y

The present invention provides a series of cyclin-dependent protein kinases (Cdks) inhibitors, Scutellaria flavonoid organic amine derivatives, synthesis and use thereof. The preparation method is as follows: taking Baicalein (or Wogonin) from Scutellaria baicalensis as lead compound, mixting it with formaldehyde solution and organic amine compounds based on the molar ratio of 1:1-1.2:1-1.2, adding methanol of duplicate weight than baicalein and reacting at 50-70.degree. C., filtering the sediment and washing and then drying so as to get the product with a content of not less than 97% (weight). Similar to Flavopiridol and P276-00, the activity of baicalein organic amine derivatives inhibiting Cdks has an increase of 50 times compared with that of Baicalin. It can selectively induce apoptosis of the proliferative phase cancer cells, which has scarcely any influence to the normal structure, and it belongs to anticancer drugs of cell cycle inhibitor kind. The product has a rich source of raw materials and has simple process, high purity, low cost, clear metabolic mechanism, high efficiency and low toxicity, which can be made into oral preparations or injections together with acid salts and is expected to become high efficient and low toxicity anti-cancer and AIDS drugs.

Zhang; Shixuan

Bao; Yongming

Sun; Yuming

Li; Kangjian

Zou; Liang

Ma; Jigang

Sun; Xiaodan

Shang; Haiyan

Li; Jing

Cyclin-dependent protein kinases inhibitors of Scutellaria flavonoid organic amine derivatives, synthesis and use thereof

baicalin

kansè

neoplasms

baicalin/kansè

Synthesis and use of anti-tumor drug LQC-Y

Cyclin-dependent protein kinases inhibitors of Scutellaria flavonoid organic amine derivatives, synthesis and use thereof

Baz done ki pi konplè remèd fèy medsin te apiye nan syans