A copper-catalyzed domino method for synthesis of quinazolinones has been developed using readily available α-amino acids as the nitrogen-containing motifs. The domino process underwent Ullmann-type N-arylation, decarboxylation, aerobic oxidation, and intramolecular addition. This method should provide a new and useful strategy for construction of N-heterocycles.

Amino acids as the nitrogen-containing motifs in copper-catalyzed domino synthesis of N-heterocycles.

The series of novel N-aryl(alkaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetamides were obtained by aminolysis of activated acids 1a–1d and by alkylation of potassium salts 2a–2d by N
 -aryl-2-chloroacetamies. The structures of compounds were determined by IR, 1H, 13C NMR, LC- and EI-MS analyses. The results of cytotoxicity evaluation by bioluminescence inhibition of bacterium Photobacterium leiognathi Sh1 showed that compounds reveal moderate cytotoxicity. Screening of anticancer activity in vitro yielded the most active compounds 3t, 4b, 4f, 4l and 4n in micromolar concentrations with the GI50 level (logGI50 is from −7.57 to −4.05 for different cell lines, and logGI50 mean graph midpoint varied from −5.30 to −4.50). Moreover, compound 4b had a distinctive selectivity against renal cancer, 4f—colon cancer and melanoma and 4l—renal cancer. The highest sensitivity to compound 4b showed renal cancer cell lines A498 (logGI50 = −7.57). SAR-analysis was discussed, COMPARE analysis and docking was studied. The novel synthesis methods of the N-aryl(alkaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetamides are proposed. Anticancer activity and Photobacterium leiognathi Sh1 bioluminescence inhibition of synthesized compounds are discussed. SAR-analysis was discussed, and COMPARE analysis and docking was studied.

Novel N-aryl(alkaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetamides: synthesis, cytotoxicity, anticancer activity, COMPARE analysis and docking

A one-pot I2-mediated annulation reaction of substrates containing diamino groups and aldehydes has been developed via oxidative C–N bond formation. This general and environmentally benign synthetic approach provides facile access to a variety of 1,3-diazaheterocyclic compounds, including quinazolinones, benzimidazoles, and cyclic amidines.

/pdf/metal-free-one-pot-synthesis-of-1-3-diazaheterocyclic-5b0g5uwx3t.pdf

Metal-free one-pot synthesis of 1,3-diazaheterocyclic compounds via I2-mediated oxidative C–N bond formation

Synthesis and Antifungal Activity of Novel Quinazolin-4(3H)-one Derivatives

Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents.

A new series of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones were synthesized via a five-steps procedure starting from 2-amino-5-methylbenzoic acid. The cytotoxicity of the resulting compounds against A-549 (human lung cancer), HCT-8 (human colon cancer), HepG2 (human liver cancer), and K562 (human myelogenous leukaemia) cell lines was determined by the MTT assay. Preliminary screening results of these compounds are reported.

Synthesis and cytotoxicity screening of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones.

The title compounds, 4-(3-nitropyridin-2-ylamino)phenol (I) and 4-(3-aminopyridin-2-ylamino)phenol (II), are two intermediates for the synthesis of a potential antitumor agent ABT-751. The reaction of 4-aminophenol with 2-chloro-3-nitropyridine yielded I which was converted into II by reduction. Instead of the Pd/C catalytic hydrogenation described in many literature, reduction with cheap sodium sulfide in aqueous media was utilized for shorting the reaction time and simplifying the operation. The crystal structures of the resultant compounds were determined by single-crystal X-ray diffraction. The compound I is crystallized in P21/c space group of monoclinic system, with a = 11.5236(19) A, b = 8.7389(17) A, c = 10.684(3) A and α = 90.00°, β = 107.76(3)°, γ = 90.00°. The compound II is crystallized in Cc space group of monoclinic system, with a = 10.688(2) A, b = 14.2181(18) A, c = 7.9836(15) A and α = 90.00°, β = 125.801(7)°, γ = 90.00°. In both crystal structures, the intermolecular N–H–O and O–H–N hydrogen bonds link the molecules, which effectively stabilize the structures. The preparation and crystal structures of 4-(3-nitropyridin-2-ylamino)phenol and 4-(3-aminopyridin-2-ylamino)phenol are reported.

Synthesis and Crystal Structures of 4-(3-Nitropyridin-2-ylamino)phenol and 4-(3-Aminopyridin-2-ylamino)phenol

Pokemon is an important transcription factor that regulates the important tumor suppressor alternative reading frame (ARF). Pokemon is overexpressed in multiple human cancers. Lack of Pokemon causes cellular senescence, apoptosis, and blockage of differentiation. We've designed and synthesized four 18-mer phosphorothioate modified antisense oligonucleotides targeting the coding regions of Pokemon mRNA, and investigated the down-regulation of Pokemon expression by measuring the fluorescence intensity of Pokemon-GFP fusion protein in COS-7 cells. Antisense oligonucleotide As4, targeting 1496–1513 sites of Pokemon mRNA, has been proven as the most potent compound and down-regulates the expression of Pokemon-GFP fusion protein to 22% at 40 nmol/L for 24 h.

Inhibition of Pokemon Gene Expression by Antisense Oligonucleotides

Handle everyday research tasks with reliable, citation-backed results

Your personal Research Agent to handle research tasks with citation-backed results

Popular Tasks used by Researchers

How can I help with your research?

Meet SciSpace

Get more enhanced response by uploading the PDFs you want me to reference.

No relevant PDFs in your library

SciSpace is the AI research assistant for academics. Run systematic literature reviews on 280M+ papers, and write papers with cited sources. Trusted by 1M+ students, PhDs & researchers.

SciSpace | AI for Research

Analyze PDFs

Code & Manuscripts

Funding & Grants

Literature & Patents

Medical & Clinical Data

Systematic Review

Visualize & Present

Web & Data

Build a Google Scholar-like website for your research.

Build a website

Create charts and images for your research

Create a Chart

Write a paper for submission to a journal

Draft a manuscript

Patent Search

Design eye-catching scientific posters in minutes.

Scientific Poster Generation

Systematic Literature Review

One task is running at the moment. Your messages will be shown right after.

Drag and drop or click here to browse

Loved by <highlight>1 million+</highlight> researchers

Extract a list of specific topics and their sources from unstructured text

Topics

Compare and analyze relevant papers that matches with your search

Papers

Get insights from PDFs and bookmarked papers from your library

My library

Recent searches

Try searching for:

Catch AI-generated content in scholarly and non-scholarly content

{ai} Detector

Ai Writer

Get PDF Summaries, highlighted text explanations 

Chat with PDF

Effortlessly create in-text citations and bibliographies in APA and 2,500 other formats

Citation generator

Get explanations, summaries, and answers on academic papers

Ease up your research workflow with {scispace}'s cohort of exciting AI tools

Elevate your academic writing skills and convey your ideas the way you want

Paraphraser

Explore our range of reading and writing tools

Your file is being prepared and should be ready in a few minutes. If it's a large file, it might take a bit longer. You can close this window, and we'll email you the file when it's done.

You have reached a maximum limit of <strong>{limit}</strong> columns in the table. Remove at least <strong>1</strong> column to add or create another one.

Yue Wang

Author Tools

Chat about Author

Papers

Synthesis and cytotoxicity screening of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones.

Synthesis and Crystal Structures of 4-(3-Nitropyridin-2-ylamino)phenol and 4-(3-Aminopyridin-2-ylamino)phenol

Inhibition of Pokemon Gene Expression by Antisense Oligonucleotides