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1.
Bioprocess Biosyst Eng ; 45(9): 1581-1593, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35932338

RESUMEN

Chlorophenols are widely used in industry and are known environmental pollutants. The degradation of chlorophenols is important for environmental remediation. In this study, we evaluated the biodegradation of 2-chlorophenol using crude laccase produced by Myrothecium verrucaria. Atmospheric and room temperature plasma technology was used to increase laccase production. The culture conditions of the M-6 mutant were optimized. Our results showed that corn stover could replace glucose as a carbon source and promote laccase production. The maximum laccase activity of 30.08 U/mL was achieved after optimization, which was a 19.04-fold increase. The biodegradation rate of 2-chlorophenol using crude laccase was 97.13%, a positive correlation was determined between laccase activity and degradation rate. The toxicity of 2-CP was substantially reduced after degradation by laccase solution. Our findings show the feasibility of the use of corn stover in laccase production by M. verrucaria mutant and the subsequent biodegradation of 2-chlorophenol using crude laccase.


Asunto(s)
Clorofenoles , Lacasa , Biodegradación Ambiental , Carbono , Clorofenoles/metabolismo , Hypocreales , Zea mays
2.
J Org Chem ; 86(23): 16916-16925, 2021 12 03.
Artículo en Inglés | MEDLINE | ID: mdl-34753287

RESUMEN

We herein report an I2/CuCl2-copromoted diamination of C(sp3)-H bonds for the preparation of 2-acyl-4-aminoquinazolines from methyl ketones, 2-aminobenzonitriles, and ammonium acetate. This reaction features operational simplicity, commercially available substrates, mild reaction conditions, and good functional group compatibility. Mechanistic studies indicate that CuCl2 plays a pivotal role in this transformation. This study uses a methyl group as a novel input to construct 2-acyl-4-aminoquinazoline derivatives for the first time.


Asunto(s)
Cetonas , Acetatos , Catálisis , Ciclización , Estructura Molecular , Nitrilos , Quinazolinas
3.
J Org Chem ; 86(12): 8381-8388, 2021 Jun 18.
Artículo en Inglés | MEDLINE | ID: mdl-34106703

RESUMEN

A novel I2-mediated Povarov reaction of arylacetylenes and anilines for the synthesis of 2,4-substituted quinolines has been developed, in which arylacetylene first acts as both a diene precursor and dienophile. This work further develops the Povarov reaction to expand the types of diene precursors. Preliminary mechanistic studies indicate that the I2/DMSO system realized the oxidative carbonylation of C(sp)-H of arylacetylene and then undergoes a [4 + 2] cycloaddition reaction.

4.
J Org Chem ; 86(17): 12141-12147, 2021 09 03.
Artículo en Inglés | MEDLINE | ID: mdl-34479411

RESUMEN

A novel iodine promoted cyclization of enaminone with aryl methyl ketones has been developed as a straightforward method for constructing 2-hydroxy-pyrrol-3(2H)-ones. This strategy affords structurally diverse 2-hydroxy-pyrrol-3(2H)-ones rings in high yields. Moreover, a quarternary alcohol has been constructed efficiently in the reaction. Product purification required only washing with CH2Cl2 solvent, thereby avoiding traditional chromatography and recrystallization, making this an example of group-assisted purification chemistry.


Asunto(s)
Yodo , Carbono , Ciclización , Reacción de Cicloadición , Estructura Molecular
5.
J Org Chem ; 86(19): 13664-13672, 2021 10 01.
Artículo en Inglés | MEDLINE | ID: mdl-34519212

RESUMEN

We herein report an iodine-mediated formal [2 + 2 + 1] cyclization of methyl ketones, p-toluenesulfonyl hydrazines, and 1-aminopyridinium iodide for preparation of 4-aryl-NH-1,2,3-triazoles under metal- and azide-free conditions. Notably, this is achieved using p-toluenesulfonyl hydrazines and 1-aminopyridinium iodide as azide surrogates, providing a novel route toNH-1,2,3-triazoles. Furthermore, this approach provides rapid and practical access to potent inhibitors of indoleamine 2,3-dioxygenase (IDO).


Asunto(s)
Azidas , Triazoles , Catálisis , Ciclización , Yoduros
6.
Blood Sci ; 5(4): 221-236, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37941914

RESUMEN

Multiple myeloma (MM) is a malignant neoplasm characterized by clonal proliferation of abnormal plasma cells. In many countries, it ranks as the second most prevalent malignant neoplasm of the hematopoietic system. Although treatment methods for MM have been continuously improved and the survival of patients has been dramatically prolonged, MM remains an incurable disease with a high probability of recurrence. As such, there are still many challenges to be addressed. One promising approach is single-cell RNA sequencing (scRNA-seq), which can elucidate the transcriptome heterogeneity of individual cells and reveal previously unknown cell types or states in complex tissues. In this review, we outlined the experimental workflow of scRNA-seq in MM, listed some commonly used scRNA-seq platforms and analytical tools. In addition, with the advent of scRNA-seq, many studies have made new progress in the key molecular mechanisms during MM clonal evolution, cell interactions and molecular regulation in the microenvironment, and drug resistance mechanisms in target therapy. We summarized the main findings and sequencing platforms for applying scRNA-seq to MM research and proposed broad directions for targeted therapies based on these findings.

7.
Org Lett ; 24(24): 4449-4453, 2022 Jun 24.
Artículo en Inglés | MEDLINE | ID: mdl-35696662

RESUMEN

A novel multicomponent cascade cyclization and sulfenylation/selenation using aryl methyl ketones, isoquinolin-1-amine, and sodium arylsulfinates/1,2-diphenyldiselane to synthesize imidazo[2,1-a]isoquinoline derivatives in one-pot via the construction of two C-N bonds and one C-S/C-Se bond has been reported. This multicomponent reaction realizes simultaneous C(sp3)-H amination and sulfenylation/selenation, avoiding complicated prior substrate preparation. This process has simple operating conditions and good substrate compatibility.

8.
Org Lett ; 23(16): 6461-6465, 2021 Aug 20.
Artículo en Inglés | MEDLINE | ID: mdl-34346696

RESUMEN

A novel [2 + 1 + 3] cyclization reaction for the synthesis of 2-aryl-4-quinolinecarboxylates from aryl methyl ketones, arylamines, and 1,3-dicarbonyl compounds has been established. This metal-free process achieved the C-C bond cleavage of 1,3-dicarbonyl compounds directly as a single-carbon synthon. The reaction is highly efficient and has good substrate compatibility while operating under mild conditions. This method has good practicability and successfully realized the synthesis of bioactive molecules.

9.
Chem Commun (Camb) ; 56(83): 12554-12557, 2020 Oct 25.
Artículo en Inglés | MEDLINE | ID: mdl-32940307

RESUMEN

The first synthesis of eight-membered N-containing heterocycles by oxidative bicyclization/ring extension of arylacetylenes and aryl amines has been achieved. This protocol uses arylacetylene as an unusual two-carbon synthon by incorporating the two parts of the cracked C[triple bond, length as m-dash]C bond into the final product, which provides a new method for using arylacetylenes as two-carbon synthons and further enriches C[triple bond, length as m-dash]C bond cleavage methodology. Moreover, this multi-component reaction can provide diverse fused elegant eight-membered N-heterocycles under mild conditions with wide substrate scopes.

10.
Org Lett ; 22(21): 8528-8532, 2020 Nov 06.
Artículo en Inglés | MEDLINE | ID: mdl-33047965

RESUMEN

A novel and efficient multicomponent cyclization of methyl ketones, cyanamides, and arylamines for the synthesizing 2,4-diamino-1,3,5-triazines via consecutive formation of four C-N bonds is reported. This multicomponent reaction is characterized by the employment of two molecules of cyanamide for double C(sp3)-H amination of methyl ketones, avoiding complicated prepreparation of substrates and expanding the substrate scope. Furthermore, this multicomponent cyclization strategy provides a new approach for generating diverse 2,4-diamino-1,3,5-triazines with a broad substrate scope under mild conditions.

11.
Org Lett ; 22(21): 8359-8364, 2020 11 06.
Artículo en Inglés | MEDLINE | ID: mdl-33040530

RESUMEN

A novel method for the synthesis of 5H-benzo[a]fluoren-5-one from inactive nonterminal 1,6-alkynes through a free radical tandem bicyclization process has been established. This process achieved a continuous cyclization triggered rarely by the α-position of α,ß-unsaturated ketones. The reaction constructed three C-C bonds in one step with the readily accessible substrates and excellent substrate compatibility.

12.
Org Lett ; 22(18): 7103-7107, 2020 09 18.
Artículo en Inglés | MEDLINE | ID: mdl-32877200

RESUMEN

The first synthesis of arylquinazolinones has been disclosed via the consecutive oxidative cyclization/ring-opening of anilines and methyl ketones. This transformation is characterized by the splitting of the methyl ketone as acyl and C1 sources through C(CO)-C(sp3) bond cleavage, using DMSO as a C1 source via C-S bond cleavage, which expands the use of methyl ketones as valuable building blocks and enriches the library of preparation quinazolinones. Moreover, preliminary mechanistic studies indicate that this multicomponent reaction underwent a consecutive cyclization/ring-opening sequence.

13.
Exp Ther Med ; 9(2): 543-546, 2015 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-25574231

RESUMEN

The aim of the present study was to investigate the correlation between nuclear factor-κB (NF-κB) activity and pulmonary artery pressure in the pulmonary artery endothelial cells of high pulmonary blood flow rat models. A total of 50 four-week-old male Wistar rats were randomly divided into four groups: Surgery shunt group (Tn, n=15); surgery + pyrollidine dithiocarbamate (PDTC) administration group (Ti, n=15); sham control group (Co, n=10) and negative control group (Cn, n=10). The 30 rats of the Ti and Tn groups underwent carotid artery-external jugular vein anastomosis; the 15 rats in the Ti group were injected with PDTC intraperitoneally 1 h prior to surgery for a two-week continuous infusion. After 12 weeks of feeding ad libitum, right ventricular systolic pressure and NF-κB activity in the pulmonary artery endothelial cells of the rats were measured. The NF-κB activity of the Tn group was significantly higher than that of the Cn group (P<0.01) and the NF-κB activity of the Ti group was lower than that of the Cn group (P<0.01); however, no significant difference was observed between the Co and Cn groups. The increased activity of NF-κB was an important factor in the pulmonary vasoconstriction and structural remodeling of rats with high pulmonary blood flow.

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