1584301-48-3

Upstream product

• 1584301-40-5 C₁₀H₁₂N₂O₄ 
• 104916-29-2 1-Acetyl-4-(1-pyrrolidinyl)-1,2,3,6-tetrahydro-pyridine 
• 32161-06-1 1-acetyl-4-piperidinone 
• 1184181-48-3 2,4-dihydroxy-5- isopropylbenzoic acid 

Downstream Products

• 1584301-56-3 5-(2,4-dihydroxy-5-isopropylbenzoyl)-N-ethyl-4,5,6,7-tetrahydroisoxazole[4,5-c]pyridine-3-carboxamide 

Relevant academic research and scientific papers

Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites

A set of compounds, previously selected as potent Hsp90α inhibitors, has been studied on a panel of human parasites. 5-Aryl-3,4-isoxazolediamide derivatives (1) were active against two protozoa, Trypanosoma brucei rhodesiense and Plasmodium falciparum, with a good tolerability toward cytotoxicity on non-malignant L6 rat myoblast cell line, unlike the 1,5-diaryl,4-carboxamides-1,2,3-triazole derivatives (2) which, while showing a single-digit nM range activity against the same protozoa, were also highly cytotoxic on L6 cells. In a subsequent in vivo study, two isoxazolediamide derivatives, 1a and 1b, were very efficacious on the sleeping sickness-causing agent with a clear parasitaemia during treatment. These data, however, showed that not all protozoa are sensitive to Hsp90 inhibitors, as well as not all Hsp90 inhibitors are equally active on parasites.

4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors

Hsp90 is considered an interesting therapeutic target for anticancer drug development. Here we describe a new class of 4,5,6,7-tetrahydro-isoxazolo-[4,5- c]-pyridine compounds. A small library of derivatives has been synthesized and investigated. Some reported compounds show interesting properties combining both notable binding to Hsp90 and potent cell growth inhibitory activity. N-5 substitution with a 2,4 resorcinol carboxamide appears crucial for activity. Moreover, a derivative bearing a hydroxamic acid residue bound to C-3 amide portion was found to inhibit both Hsp90 and HDAC6.