1024592-54-8

Usage

Uses

1. Used in Pharmaceutical Industry:
BenzaMide, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-4,5-dimethoxy-2-nitrois used as an intermediate in the synthesis of Tariquidar (T007600) for the following reasons:
a. Tariquidar is a P-glycoprotein drug efflux pump inhibitor, which plays a crucial role in the development of multidrug resistance in cancer cells. By inhibiting this pump, Tariquidar can increase the effectiveness of chemotherapeutic drugs and potentially improve treatment outcomes for cancer patients.
b. The compound's unique chemical structure allows it to be a key component in the synthesis of Tariquidar, contributing to its overall pharmacological properties and efficacy.
2. Used in Cancer Treatment:
BenzaMide, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-4,5-dimethoxy-2-nitrois used as a precursor in the development of cancer treatment options, specifically through its role in the synthesis of Tariquidar. The application reason is as follows:
a. As a P-glycoprotein inhibitor, Tariquidar can help overcome multidrug resistance in cancer cells, allowing for more effective treatment with conventional chemotherapeutic agents.
b. The compound's involvement in the synthesis of Tariquidar highlights its potential contribution to the development of novel cancer therapies and the improvement of existing treatment options.

Upstream product

• 4998-07-6 4,5-dimethoxy-2-nitro-benzoic acid 
• 82925-02-8 4-<2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolyl)ethyl>benzenamine 
• 82925-01-7 1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[2-(4-nitrophenyl)ethyl]-isoquinoline 
• 5339-26-4 (4-nitrophenyl)ethyl bromide 
• 1745-07-9 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline 
• 29568-78-3 4,5-dimethoxy-2-nitrobenzoyl chloride 

Downstream Products

• 849668-91-3 2-amino-N-{4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-phenyl}-4,5-dimethoxybenzamide 

Relevant academic research and scientific papers

DEUTERATED ANALOGS OF TARIQUIDAR

The present invention relates to efflux inhibitor compounds, compositions, and methods of using the same. More specifically, the instant invention comprises deuterated analogs of tariquidar with superior pharmacokinetic properties such that it is now poss

Reversal of P-gp and BCRP-mediated MDR by tariquidar derivatives

Abstract With an aim to generate non-toxic, specific and highly potent multidrug resistance (MDR) modulators, a novel series of anthranilic acid amide-substituted tariquidar derivatives were synthesized. The new compounds were evaluated for their cytotoxicity toward normal human colon fibroblasts (CCD18-Co), human gastric epithelial cell line (HFE) and primary rat liver cells, and for their ability to inhibit P-gp/BCRP-mediated drug efflux and reversal of P-gp and BCRP-mediated MDR in parental and drug-resistant cancer cell lines (LCC6 MDR1, MCF-7 FLV1000, R-HepG2, SW620-Ad300). While tariquidar is highly toxic to normal cells, the new derivatives exhibited much lower or negligible cytotoxicity. Some of the new tariquidar derivatives inhibited both P-gp and BCRP-mediated drug efflux whereas a few of them bearing a sulfonamide functional group (1, 5, and 16) are specific to P-gp. The new compounds were also found to potentiate the anticancer activity of the transporter substrate anticancer drugs in the corresponding transporter-overexpressing cell lines. The extent of resistance reversal was found to be consistent with the transporter inhibitory effect of the new derivatives. To further understand the mechanism of P-gp and BCRP inhibition, the tariquidar derivatives were found to interact with the transporters using an antibody-based UIC2 or 5D3 shift assay. Moreover, the transporters-inhibiting derivatives were found to modulate the ATPase activities of the two MDR transporters. Our data thus advocate further development of the new compounds for the circumvention of MDR.

Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators

The development of new modulators possessing high efficacy, low toxicity and high selectivity is a pivotal approach to overcoming P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in tumour cells. In this study 39 compounds are presented which hav

NOVEL P-GLYCOPROTEIN INHIBITOR, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

A p-glycoprotein inhibitor of Formula 1 is capable of effectively preventing the development of multi-drug resistance directed to an anticancer agent in cancer cells, and greatly enhances the bioavailability of the drug, such as paclitaxel, which is not readily absorbed when orally administered.