1269418-45-2

Upstream product

• 42021-12-5 dl-methyl-1,2,3,4-tetrahydro-9H-pyrido-<3,4-b>indole-3-carboxylate hydrochloride 
• 7524-52-9 (S)-tryptophan methyl ester hydrochloride 
• 6052-68-2 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid 
• 42021-11-4 methyl 1,2,3,4-tetrahydro-β-carboline-3-carboxylate 
• 73834-77-2 3-amino-9H-β-carboline 
• 1269418-57-6 N-(β-carbolin-3-yl)cyclohexanecarboxamide 

Relevant academic research and scientific papers

Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents

So far, relatively few small molecules have been reported to promote tubulin degradation. Our previous studies have found that compound 2, a noncovalent colchicine-site ligand, was capable of promoting αβ-tubulin degradation. To further improve its antipr

Carboline derivative/analogue as well as preparation method and application thereof

The invention belongs to the field of chemical medicines, and provides a compound shown as a formula I or pharmaceutically acceptable salt thereof. The invention also provides analogues of the compound as shown in the formula I in the specification. Biological experiments show that the compound disclosed by the invention has anti-tumor activity and serves as a good tubulin inhibitor; the compound91b has excellent antitumor activity, can effectively promote degradation of tubulin; drug resistance caused by overexpression of beta-tubulin III and P-gp can be eliminated, and a new choice is provided for clinical medication.

3-Benzylamino-β-carboline derivatives induce apoptosis through G 2/M arrest in human carcinoma cells HeLa S-3

β-Carboline derivatives are known as the lead compounds for anti-tumor agents. To examine an optimal structure for anti-tumor activity, we synthesized a variety of β-carboline derivatives, possessing a variety of substituents on the nitrogen atom of the amino group of 3-amino-β-carboline, and evaluated their anti-tumor activity for HeLa S-3 cell line. 3-(4,5- Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay showed that an optimal structure for anti-tumor activity was 3-cyclohexylmethylamino (1e) or 3-benzylamino-β-carboline (1f). An optimal counter anion of 2-methyl-3-benzylamino- β-carbolinium salts was a triflate anion 2c. In addition, the introduction of a hydroxyl group on the meta-position of the benzyl group of 3-benzylamino-β-carboline (3e) enhanced its anti-tumor activity. Hoechst 33342 staining and DNA fragmentation assay suggested that 1f, 2c and 3e induced cell death by apoptosis unlike 1e. Flow cytometry analysis showed that 1f, 2c and 3e induced cell apoptosis through arrest of the cell cycle in the G2/M phase.