51707-38-1Relevant articles and documents
Hydrazide compounds
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, (2019/10/01)
The invention discloses hydrazide compounds. The compounds are characterized by having a structure represented by a formula I shown in the description, wherein Ar1 and Ar2 are each independently selected from the group consisting of aryl, azinyl, piperazinyl, pyrazolyl, imidazolyl, pyrrolyl, phenyl, naphthyl, thiazolyl, thienyl, furyl, aryl, phenyl, piperazinyl, piperidinyl, piperazinyl, and-C13H9represented by a formula 9 shown in the description, only one of the Ar1 and the Ar2 is phenyl, the Ar1 has m substituents R1, Ar2 has n substituents R2, m=0 to 3, and n=0 to 3; and if the formula Ihas a plurality of substituents R1 and R2, the plurality of substituents R1 and R2 are independent with one another, can select the same substituents or different substituents, and the R1 and the R2 are each independently selected from the group consisting of halogen, hydroxyl, cyano, C1-C3 alkyl, C1-C3 alkoxy, amino, C1-C3 alkyl substituted amino, C1-C3 alkyl disubstituted amino, perfluoro C1-C3alkyl and fluoro substituted C1-C3 alkoxy.
Synthesis, pharmacological evaluation and docking study of a new modulator of microtubule polymerization
Carneiro, Teiliane R.,do Amaral, Daniel N.,Fokoue, Harold H.,Sant’Anna, Carlos M. R.,Porras, Maria L. G.,Oliveira, Augusto C. A.,Cavalcanti, Bruno C.,Pessoa, Cláudia,Barreiro, Eliezer J.,Lima, Lídia M.
, p. 778 - 786 (2018/09/10)
Objectives: The main goal of this paper was to conduct the synthesis to determine cytotoxic activity and to carry out docking studies on new LASSBio-1586 isosteres. LASSBio-1586 is a new combretastatin A4 (CA4) analogue previously identified as a simple antitumor drug candidate, able to inhibit microtubule polymerization with broad in vitro and in vivo cytotoxic activity. Methods: The new isosteres (7b-7h, 8a and 9a) were evaluated against HL-60, OVCAR-8, HCT8 and LUCENA tumor cell lines, using cytotoxic test of MTT. The tubulin polymerization assay was performed using a tubulin polymerization assay kit from cytoskeletonR and by CEREP employing a single concentration of 10 μM. Binding mode at β-tubulin colchicine binding site was stablished by blind molecular docking studies. Results: LASSBio-1920 (7h) was identified as the most potent cytotoxic compound with IC50 values ranging from 0.75 nM to 11.5 nM, although it was inactive against MDR tumor cell line LUCENA (IC50 = 80 μM). This compound presented remarkable cytotoxic selective index in comparison with CA4 and LASSBio-1586. Its ability to modulate microtubule polymerization was confirmed and its mode of interaction with colchicine binding site in β-tubulin was demonstrated. Conclusion: Compound 7h is a new isostere of LASSBio-1586 that displayed potent cytotoxic activity and better cytotoxic selectivity index and has been shown to interact with DAMA-colchicine in its co-crystal with β-tubulin.
Method for synthesizing aryl formaldehyde compound from aryl formate compound
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Paragraph 0039-0041, (2017/07/06)
The invention discloses a method for synthesizing an aryl formaldehyde compound from an aryl formate compound. The method comprises the following steps: taking the aryl formate compound as a raw material, and reacting under the action of excessive hydrazine hydrate; after the end of the reaction, standing, cooling, filtering and washing, thus respectively obtaining filtrate and filter cake, wherein the filtrate is the hydrazine hydrate, and the filter cake is an aryl formylhydrazine compound; recycling and reusing the filtrate; then dissolving the aryl formylhydrazine compound in a solvent, reacting under the existence of 2-iodoxybenzoic acid and alkali, and carrying out aftertreatment, thus obtaining the aryl formaldehyde compound and a byproduct-2-iodosobenzoic acid; regenerating the 2-iodoxybenzoic acid after oxidizing the 2-iodosobenzoic acid, and repeatedly using the 2-iodoxybenzoic acid. According to the method disclosed by the invention, recycling and cyclic utilization of materials are fully realized, emissions are less, environment friendliness is realized, and the yield is higher.