1427018-99-2Relevant academic research and scientific papers
Synthesis and in vitro antitumor activity of novel bivalent β-carboline-3-carboxylic acid derivatives with DNA as a potential target
Gu, Hongling,Li, Na,Dai, Jiangkun,Xi, Yaxi,Wang, Shijun,Wang, Junru
, (2018)
A series of novel bivalent β-carboline derivatives were designed and synthesized, and in vitro cytotoxicity, cell apoptosis, and DNA-binding affinity were evaluated. The cytotoxic results demonstrated that most bivalent β-carboline derivatives exhibited stronger cytotoxicity than the corresponding monomer against the five selected tumor cell lines (A549, SGC-7901, Hela, SMMC-7721, and MCF-7), indicating that the dimerization at the C3 position could enhance the antitumor activity of β-carbolines. Among the derivatives tested, 4B, 6i, 4D, and 6u displayed considerable cytotoxicity against A549 cell line. Furthermore, 4B, 6i, 4D, and 6u induced cell apoptosis in a dose-dependent manner, and caused cell cycle arrest at the S and G2/M phases. Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with β-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. In addition, the results of UV-visible spectral, thermal denaturation, and molecular docking studies revealed that 4B, 6i, 4D, and 6u could bind to DNA mainly by intercalation.
Β - Carboline -3 - carboxylic acid dimer for preparing the prevention and treatment of anti-lung cancer drug application (by machine translation)
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Paragraph 0027; 0030; 0033; 0034, (2019/02/13)
The present invention relates to β - Carboline - 3 - carboxylic acid dimer of the new application, in particular to β - Carboline - 3 - carboxylic acid dimer for preparing the prevention and treatment of anti-lung cancer drug application, this invention stated β - Carboline - 3 - carboxylic acid dimer of the anti-lung cancer cell activity higher than the activity of anti-other cancer cells. (by machine translation)
3 dual-position double-β - Carboline alkali compound, its preparation and its pharmaceutical composition and use thereof
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Paragraph 0203-0207, (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.
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
supporting information, p. 953 - 957 (2014/07/08)
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.
