1427019-04-2Relevant articles and documents
Synthesis and biological evaluation of novel bivalent β-carbolines as potential antitumor agents
Wu, Qifeng,Bai, Zhushuang,Ma, Qin,Fan, Wenxi,Guo, Liang,Zhang, Guoxian,Qiu, Liqin,Yu, Huijuan,Shao, Guang,Cao, Rihui
, p. 953 - 957 (2014)
A series of novel bivalent β-carbolines with a spacer of three to ten methylene units between the 3-carboxyl oxygens was synthesized and evaluated as antitumor agents. The results demonstrated that most compounds displayed good and selective cytotoxic activities against 769-P and KB cell lines. Acute toxicities and antitumor efficacies of the selected compounds in mice were also evaluated. Compound 22 exhibited potent antitumor activity against Lewis lung cancer in mice with a tumor inhibition rate of 64.2%. Preliminary structure-activity relationship analysis indicated that (1) the length of the spacer affected cytotoxic activities in vitro and six methylene units were more favorable; (2) the introduction of substituents into position-1 of the β-carboline ring might be detrimental to antitumor potency in vivo models.
3 dual-position double-β - Carboline alkali compound, its preparation and its pharmaceutical composition and use thereof
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Paragraph 0222-0226, (2017/08/29)
The invention discloses a bis-beta-carboline alkali compound, and a preparation method, a pharmaceutical composition and application thereof. Specifically, the bis-beta-carboline alkali compound and a pharmaceutically acceptable salt thereof are shown in the general formula I. The bis-beta-carboline alkali compound is prepared by condensation of beta-carboline intermediates and dihaloalkane hydrocarbons. The invention further discloses a pharmaceutical composition and application of the bis-beta-carboline alkali compound in preparing anti-tumor drugs. The pharmaceutical composition comprises an effective dose of bis-beta-carboline alkali compound shown in the formula I and a pharmaceutically acceptable carrier, and the tumor comprises melanoma, gastric cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer and colon cancer.