54780-94-8

Upstream product

• 302-79-4 all-trans-retinoic-acid 
• 134394-00-6 C₂₃H₃₂O₄ 

Relevant academic research and scientific papers

An expeditious hydroxyamidation of carboxylic acids

Capitalizing on in situ activation with the cyclic phosphonic anhydride PPAA (1), the conversion of carboxylic acids into hydroxamic acids has been reduced to an experimentally simple one-pot operation that addresses the issue of polyacylation without resorting to a large excess of hydroxylamine or to protection. Scope and selectivity were satisfactory with a wide range of substrates, including α,β-unsaturated acids and hydroxyacids.

A class of tretinoin N-hydroxyamide derivatives, preparation method and applications thereof

The present invention relates to a class of tretinoin N-hydroxyamide derivatives, and a preparation method thereof, and applications of the tretinoin N-hydroxyamide derivatives as tumor treatment drugs and biochemical reagents. According to the present invention, three tretinoin isomers are used as raw materials and are subjected to a two-step synthesis reaction so as to prepare the tretinoin N-hydroxyamide derivatives; and the compounds can provide significant anti-proliferation and apoptosis promoting effects on tumor cells while provide low toxicity to normal cells, such that the compoundshave potential medicinal or scientific values.

N-hydroxyamide derivatives of retinoic acid and preparation and application of N-hydroxyamide derivatives of retinoic acid

The invention relates to N-hydroxyamide derivatives of retinoic acid and a preparation method of N-hydroxyamide derivatives of retinoic acid, and application of N-hydroxyamide derivatives of retinoicacid as tumor treatment drugs and biochemical reagents. The N-hydroxyamide derivative of retinoic acid is prepared by using three kinds of retinoic acid isomers as raw materials through a two-step synthesis reaction. This type of compound exhibits significant anti-proliferative and pro-apoptotic effects on tumor cells and less toxicity on normal cells, and therefore has potential medicinal or scientific value.

Small-molecule inhibitors of histone acetyltransferase activity: Identification and biological properties

Starting from a yeast phenotypic screening performed on 21 compounds, we described the identification of two small molecules (9 and 18) able to significantly reduce the S. cerevisiae cell growth, thus miming the effect of GCN5 deletion mutant. Tested on a GCN5-dependent gene transcription assay, compounds 9 and 18 gave a high reduction of the reporter activity. In S. cerevisiae histone H3 terminal tails assay, the H3 acetylation levels were highly reduced by treatment with 0.6-1 mM 9, while 18 was effective only at 1.5 mM. In human leukemia U937 cell line, at 1 mM 9 and 18 showed effects on cell cycle (arrest in G1 phase, 9), apoptosis (9), and granulocytic differentiation (18). When tested on U937 cell nuclear extracts to evaluate their histone acetyltransferase (HAT) inhibitory action, both compounds were able to reduce the enzyme activity when used at 500 μM. Another quinoline, compound 22, was synthesized with the aim to improve the activity observed with 9 and 18. Tested in the HAT assay, 22 was able to reduce the HAT catalytic action at 50 and 25 μM, thereby being comparable to anacardic acid, curcumin, and MB-3 used as references. Finally, in U937 cells, compounds 9 and 18 used at 2.5 mM were able to reduce the extent of the acetylation levels of histone H3 (9) and α-tubulin (9 and 18). In the same assay, 22 at lower concentration (100 μM) showed the same hypoacetylating effects with both histone and non-histone substrates.