129716-58-1

Usage

Uses

Used in Oncology:
Dofequidar is used as a P-glycoprotein inhibitor for the purpose of reversing multidrug resistance in cancer cells. By doing so, it allows chemotherapy drugs to penetrate and accumulate within cancer cells more effectively, which can lead to improved treatment efficacy for patients with cancers that have developed resistance to standard chemotherapy regimens.
Used in Cancer Treatment Research:
In the field of cancer treatment research, dofequidar is utilized as a subject of study to explore its potential in overcoming drug resistance in cancer. This research is crucial for understanding the compound's benefits and limitations, and for developing strategies to enhance the effectiveness of existing chemotherapy drugs in treating drug-resistant cancers.

InChI:InChI=1/C30H31N3O3/c34-25(22-36-28-15-7-14-27-26(28)13-8-16-31-27)21-32-17-19-33(20-18-32)30(35)29(23-9-3-1-4-10-23)24-11-5-2-6-12-24/h1-16,25,29,34H,17-22H2

Upstream product

• 67199-13-7 N-(2,2-diphenylacetyl)piperazine 
• 67199-20-6 1-Diphenylacetyl-4-formylpiperazine 
• 129717-21-1 R-1-(5-quinolinyloxy)-2,3-epoxypropane 
• 1871-76-7 diphenylacetic acid chloride 
• 578-67-6 quinolin-5-ol 

Downstream Products

• 222054-83-3 methyl 1-O-<(S)-3-<4-(2,2-diphenylacetyl)piperazin-1-yl>-1-(quinolin-5-yloxy)-2-propyl>-2,3,4-tri-O-pivaloyl-β-D-glucuronate 
• 222054-82-2 methyl 1-O-<(R)-3-<4-(2,2-diphenylacetyl)piperazin-1-yl>-1-(quinolin-5-yloxy)-2-propyl>-2,3,4-tri-O-pivaloyl-β-D-glucuronate 
• 153653-30-6 rac-1-{4-[2-hydroxy-3-(5-quinolinyloxy)propyl]piperazin-1-yl}-2,2-diphenylethan-1-one fumarate 

Relevant academic research and scientific papers

METHOD FOR PRODUCING THE PUREST RAC-1-{4-[2-HYDROXY-3-(5-QUINOLYLOXY)PROPYL] PIPERAZIN-1-YL}-2,2-DIPHENYLETHAN-1-ONE FUMARATE AND THE PUREST RAC-1-{4-[2-HYDROXY-3-(5-QUINOLYLOXY)PROPYL]PIPERAZIN-1-YL}-2,2-DIPHENYLETHAN-1-ONE FUMARATE

The invention relates to a method for producing the purest rac-1-{4-[2-hydroxy-3-(5-quinolyloxy)propyl] piperazin-1-yl}-2,2-diphenylethan-1-one fumarate and the purest rac-1-{4-[2-hydroxy-3-(5-quinolyloxy)propyl]piperazin-1-yl}-2,2-diphenylethan-1-one fum

Structure-activity relationship of newly synthesized quinoline derivatives for reversal of multidrug resistance in cancer

The effect of 24 newly synthesized quinoline derivatives on tumor cell multidrug resistance (MDR) was examined in vitro. At low concentrations, these compounds enhanced the accumulation of [3H]vincristine in K562/ADM cells and reversed tumor cell MDR. The results of the structure-activity relationship analysis indicate that in highly active compounds the two aryl rings in the hydrophobic moiety deviate from a common plane, so they are capable of interacting with hydrogen bond donors of P-170 glycoprotein (P- gp) via π-hydrogen-π interactions. Other major structural features which influence the MDR-reversing activities of these compounds are a quinoline nitrogen atom and a basic nitrogen atom in piperazine. Furthermore, in highly active compounds, the distance between the hydrophobic moiety and the basic nitrogen atom (an atom connected to 2-hydroxypropoxyquinoline) must be at least 5 A?. Several compounds were found to reverse vincristine resistance in K562/ADM cells in vitro, and compound 16 (MS-209) was selected for clinical studies.

Quinoline derivative fumarates

Compounds having an activity to stimulate the carcinostatic effect of carcinostatic agents, which can be expressed by the following general formula (1): STR1 in which A is STR2 (in which R1, R2 and R3 are each independent

Quinoline derivatives

Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.