79610-23-4

Usage

InChI:InChI=1/C18H14N2OS3/c1-19-13-9-5-6-10-14(13)23-17(19)15-16(21)20(18(22)24-15)11-12-7-3-2-4-8-12/h2-10H,11H2,1H3

Upstream product

• 10574-69-3 3-benzylrhodanine 
• 55514-14-2 3-methyl-2-(methylthio)benzothiazolium tosylate 
• 149-30-4 2-thioxo-3H-1,3-benzothiazole 
• 95-51-2 o-chloroaniline 
• 615-22-5 2-methylmercaptobenzothiazole 
• 80-48-8 methyl p-toluene sulfonate 

Relevant academic research and scientific papers

Analogues of the allosteric heat shock protein 70 (Hsp70) inhibitor, MKT-077, as anti-cancer agents

The rhodacyanine, MKT-077, has antiproliferative activity against cancer cell lines through its ability to inhibit members of the heat shock protein 70 (Hsp70) family of molecular chaperones. However, MKT-077 is rapidly metabolized, which limits its use as either a chemical probe or potential therapeutic. We report the synthesis and characterization of MKT-077 analogues designed for greater stability. The most potent molecules, such as 30 (JG-98), were at least 3-fold more active than MKT-077 against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50 values of 0.4 ± 0.03 and 0.7 ± 0.2 μM, respectively). The analogues modestly destabilized the chaperone clients, Akt1 and Raf1, and induced apoptosis in these cells. Further, the microsomal half-life of JG-98 was improved at least 7-fold (t1/2 = 37 min) compared to MKT-077 (t1/2 5 min). Finally, NMR titration experiments suggested that these analogues bind an allosteric site that is known to accommodate MKT-077. These studies advance MKT-077 analogues as chemical probes for studying Hsp70s roles in cancer.

ANTI-LEISHMANIA AGENT

The present invention is to provide a new anti-leishmania agent with fewer side effects, having a high cell proliferation-inhibiting effect to leishamia protozoa, and also easy to manufacture at a low cost. A compound wherein a heterocycle with a conjugated system and a nitrogen atom and a heterocycle with a nitrogen atom and a sulfur atom are bound by a carbon chain with an ethylene group, that is a compound wherein a specific 5- to 8-membered heterocyclic ring and a specific 5-to 8-membered heterocycle having a conjugated system are bound via a vinylene group, more particularly a specific rhodacyanine dye compound is used as an active ingredient of the anti-leishmania agent.

HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS

Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.

Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity

The rhodacyanine dye MKT-077 (1), a potent antitumor agent, was found to possess strong in vitro activity against Plasmodium falciparum and a low cytotoxicity. Several new rhodacyanine dyes related to 1, containing a variety of linked heterocyclic moieties, were synthesized, and their antimalarial potencies were evaluated. The synthetic rhodacyanines were found to have EC50 values against P. falciparum in vitro in the range of 4-300 nM. Several compounds in this series have remarkable selective toxicity profiles (> 100).