Objective The present study focused to build pyridine and quinazoline rings in a single molecule and designed a new fused Pyrido[2,1-b] quinazoline to have a better pharmacological activity. Material and methods A three component, one-pot synthesis of substituted-1H-Pyrido[2,1-b] quinazoline derivatives has been described by conventional and microwave synthesis using triflic acid as catalyst. These compounds were screened for in vitro cytotoxic activity against the panel of cancer cell lines A549, NCI-H460, HT-29, HCT-15, DU-145, and HFL. Results Among the tested compounds, 11-(1-benzyl-1H-indol-3-y1)-2, 3, 4, 11-tetrahydro-1H-pyrido[2,1-b] quinazoline (4i) showed most potent cytotoxicity against A549 and NCI-H460 lung cancer cell lines with IC50 values 4.57±0.25 and 5.53±0.49 µM, respectively. Moreover, compound 4i was found to be most potent considerable cell growth inhibition with GI50 values of 2.70±0.18 and 3.24±0.40 µM against A549 and NCI-H460 cell lines, respectively. In addition, induction of apoptosis for compound 4i on A549 was investigated by morphological changes, Acridine orange/ethidium bromide (AO/EB) and DAPI staining. Furthermore, a strong anti-clonogenic effect of compound 4i on lung cancer cells was observed. The flow cytometric analysis investigation reveals that compound 4i arrests the A549 cancer cell lines at the G0/G1 phase of the cell cycle. Molecular docking were also performed on 4i, 4j, and erlotinib to predict the binding mode towards the EGFR kinase (PDB code: 1M17) and the compounds have displayed similar interactions and compared with erlotinib. Conclusion Overall, these findings could suggest that the compound 4i would be an ideal lead as an anticancer agent.

http://journal.waocp.org/article_88932_1016670a13de3e0b8cbf15e3196c24a9.pdf

Design, One Pot Synthesis and Molecular Docking Studies of Substituted-1H-Pyrido[2,1-b] Quinazolines as Apoptosis-Inducing Anticancer Agents.

A facile and efficient method for the synthesis of 2-phe- nylquinazolines has been developed from 2-aminobenzophenones and benzylamines catalyzed by ceric ammonium nitrate (CAN)- TBHP in acetonitrile. The corresponding 2-phenylquinazolines were obtained in good to excellent yields. In the realm of heterocyclic chemistry, quinazolines and their derivatives are focused targets from the perspective of synthetic organic chemists due to their broad biological and medicinal activities such as anticonvulsant, antibacte- rial, antidiabetic, anticarcinogenic and antihypertensive properties. 1 In view of the widespread therapeutic applica- tions associated with this quinazoline moiety, lot of ef- forts have been envisioned to construct the quinazoline derivatives. Numerous synthetic methods have been de- veloped to prepare the quinazoline derivatives, such as Bischler cyclization, involving the reaction of dicarbonyl compounds with diamines and the oxidative ring closure of 2-aminobenzonitrile with 3-phenylacryloyl chloride under basic conditions. 2 Kotsuki et al., reported the quinazoline synthesis via intramolecular nucleophilic substitution with indispensable o-fluorobenzaldehydes, bearing cyano or nitro substituents as activators. 3 Very re- cently Wang et al., reported an elegant synthesis of 2-phe- nylquinazolines employing molecular iodine/TBHP and also with supported copper oxide nanoparticles. 4 Truong et al. described copper-catalyzed Ullmann N-arylation coupling process to synthesize 2-phenylquinazolines from the corresponding o-iodobenzaldehydes and benzamidine hydrochloride under ligand-free conditions. 5 However many of the reported methodologies encounter drawbacks

An Efficient Protocol for the Synthesis of 2-Phenylquinazolines Catalyzed by Ceric Ammonium Nitrate (CAN)

Carbomethoxy-methylanthranilic acid was synthesized from methylanthranilic acid with methylchloroformate in presence of potassium carbonate. Cyclisationreaction of Ncarbomethoxymethylanthranilic acid was performed by heating to get N-methylisatoic anhydride. 2metholamino-N-(2’-phenylethyl) benzamidewas formed from Isatoic anhydride and phenylethyl amine. High yield of 1-methyl-3-(2’phenylethyl)-1H,3H-quinazoline-2,4-dione alkaloids were formed by condensation and cyclisation reaction between amide and methylchloroformate. The synthesis compound was identified with the help of its melting point, CNMR and HNMR spectra. KEYWORD: CNMR, HNMR, Carbomethoxy-methylanthranilic acid,quinazoline, alkaloid

http://www.iosrphr.org/papers/v4i02/Version-3/A04230104.pdf

Spectroscopic analysis on Synthesis 1-Methyl-3-(2’-Phenylethyl)- 1H,3H-Quinazoline-2,4-dione

Quinazoline and pyrimidine derivatives exhibit a wide range of therapeutic properties. This research paper is highlights the medicinal and synthetic aspects of pyrimidine and quinazoline derivatives.

/pdf/novel-chemical-synthesis-and-medicinal-aspects-of-some-26tu5knk7i.pdf

Novel Chemical synthesis and medicinal aspects of some quinazoline and pyrimidine derivatives

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.

Samiksha

Author Tools

Chat about Author

Papers

Novel Chemical synthesis and medicinal aspects of some quinazoline and pyrimidine derivatives