Novel dispirooxindole-pyrrolidine derivatives have been synthesized through 1,3-dipolar cycloaddition of an azomethine ylide generated from isatin and sarcosine with the dipolarophile ...3-(1H-indol-3-yl)-3-oxo-2-(2-oxoindolin-3-ylidene)propanenitrile, and also spiro compound of acenaphthenequinone obtained by the same optimized reaction condition. Synthesized compounds were evaluated for their antimicrobial activity and all the compounds shown significant activity. Anticancer activity was evaluated against A549 human lung adenocarcinoma cancer cell lines. Compounds 7b, 7g, 7i and 7r exhibit very good anticancer activity 62.96%, 62.03%, 67.67% and 60.22%, respectively, at the dose of 200μg/mL and compound 7i shows IC50 value in 50μg/mL.
Novel spirooxindole–pyrrolidine compounds have been synthesised through 1,3-dipolar cycloaddition of azomethine ylides generated from isatin and sarcosine or thioproline with the dipolarophile ...3-(1H-imidazol-2-yl)-2-(1H-indole-3-carbonyl)acrylonitrile under the optimised reaction condition. Synthesised compounds were evaluated for their anticancer activity against A549 human lung adenocarcinoma cancer cell line. Among the 29 tested compounds 4j, 6b and 6h showed very high activity 66.3%, 64.8% and 66.3% at 25 μg/mL concentration against A549 lung adenocarcinoma cancer cell line. These spirooxindole–pyrrolidine compounds can be promising therapeutic agents for A549 lung adenocarcinoma cancer cell line.
Novel spirooxindole–pyrrolidines have been synthesised through 1,3-dipolar azomethine ylide cycloaddition and evaluated for their anticancer activity against A549 lung adenocarcinoma cancer cell line. Synthesised compounds have shown significant activity. Display omitted
•Synthesis of novel spirooxindole–pyrrolidines by 1,3-dipolar cycloaddition.•Spirooxindole–pyrrolidines have versatile biological significance.•Synthesised compounds were tested against human A549 lung cancer cell line.•Synthesised compounds were subjected to molecular docking studies.•The synthesised compounds were displayed significant anticancer activity.
An improved and practical synthesis of substituted quinolines and bis(indolyl)methanes was achieved under microwave condition using Zn(OTf)
2 as catalyst. The synthesized compounds have been screened ...for antimicrobial and antioxidant activities.
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A highly efficient Cu-mediated route for the synthesis of fused 1,2,3triazolo1,4diazepines has been developed by azidation-cyclization of 2-bromo-N-propargylamines in a one-pot ...fashion. The key highlight of the present work is that the 2-bromo-N-propargylamines are prepared through the A3-reaction of cyclic amines such as isoquinoline and decarboxylative coupling of proline and pipecolinic acid with 2-bromo benzaldehyde and alkyne. As preliminary, these compounds were analyzed for their most probable bioactivity using various in silico tools. The recognized anti-neurodegenerative activity potential was assessed by molecular docking, AChE inhibition activity in erythrocytes and DPPH radical scavenging activity potentials possessed by the compounds. With a relative AChE inhibition activity of 97% (IC50 0.25 ± 0.02 µM), compound 5d identified as the most active compound. Druggability of these compounds also evaluated through Lipinski’s filter and other ADMET tools for the betterment of selective execution of in vitro and in vivo activities of the screened compounds cautiously.
A series of novel dispiropyrrolidines have been synthesized through 1,3-dipolar cycloaddition of an azomethine ylide generated from sarcosine and isatin with the dipolarophile ...3-benzylidene-1-methyl-pyrrolidine-2,5-dione. Their antibacterial activity was evaluated against
Bacillus subtilis NCIM 2718,
Staphylococcus aureus NCIM5021,
Salmonella typhi NCIM2501,
Pseudomonas aeruginosa NCIM 5029 and
Proteus vulgaris NCIM2813 by two fold dilution method. Compound
6e exhibits reasonably good activity and compound
6c exhibits poor activity against all the organisms. The QSAR’s were developed for all antibacterial activities. The models had either one or two descriptors (
r
2 = 0.81–0.97,
r
adj
2
=
0.75
–
0.96
,
q
2 = 0.57–0.92,
F-ratio = 12.73–162.76). Topology, shape, charge distribution and hydrophobic nature of the molecules had pronounced effect on their antibacterial activity.
A series of novel dispiropyrrolidines have been synthesized through 1,3-dipolar cycloaddition of azomethine ylide. The products exhibits good antibacterial activity and QSAR were developed for the antibacterial activities.
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Monkeypox virus (MPXV) causing multi-country outbreak-2022 is related to viruses caused outbreak-2017-2018 in West Africa. Still not fully understood which proteins of the MPXV discovered in Nigeria ...in 2017 have mutated through different lineages to the extent that it could cause a multi-country outbreak in 2022; similarly, codon usage bias, host adaptation indices, and the role of selection or mutation pressure in the mutated genes are also not fully studied. Here we report that according to the available sequence data this monkeypox virus acquires point mutations in multiple proteins in each period, and these point mutations accumulate and become a virus that can root outbreak-2022. Viruses exported from Nigeria to Singapore, Israel, and the United Kingdom in 2018-2019 were developed as evolutionary ancestors to B.1 viruses (MPXVs causing multi-country outbreak-2022) through MPXV/United States/2021/MD virus. Although these exported viruses have different amino acid mutations in different proteins, amino acid mutations in 10 proteins are common among them. The MPXV-United Kingdom-P2 virus evolved with only mutations in these 10 proteins and further evolved into MPXV/United States/2021/MD with amino acid mutations in 26 (including amino acid mutations in 10 proteins of the MPXV-United States-P2) proteins. It is noteworthy that specific amino acid mutations in these 22/26 (presence in MPXV/United States/2021/MD) proteins are present in B.1 viruses. Further, analysis of Relative Synonymous Codon Usage (RSCU), Synonymous Codon Usage Fraction (SCUF), and Effective Number of Codons (ENc) revealed codon usage bias in genes that exhibited nucleotide mutations in lineage B.1. Also, host adaptation indices analyzes such as Codon Adaptation Index (CAI), Expected-CAI (eCAI), Relative Codon Deoptimization Index (RCDI) and Expected value for the RCDI (eRCDI) analyzes reveal that the genes that demonstrated nucleotide mutations in lineage B.1 are favorable for human adaptation. Similarly, ENc-GC3s plot, Neutrality plot, and Parity Rule 2 (PR2)-bias plot analyzes suggest a major role of selection pressure than mutation pressure in the evolution of genes displaying nucleotide mutations in lineage B.1. Overall, from 2017 to 2022, MPXV's mutation and spread suggests that this virus continues to evolve through point mutation in the genes according to the available sequence data.
Cu(OTf)2 catalyzed efficient synthesis of spiropyrano3,2-bpyran-4(8H)-ones is accomplished via one-pot three component reaction between isatin, kojic acid and active methylenes. This synthetic ...protocol is operationally simple and affords product with good to excellent yields at a short reaction time. The synthesized compounds were evaluated for their tumor cell growth inhibitory activity against the human lung cancer cell line (A549) and found that 13 compounds exhibited moderate to good anticancer potency. Molecular docking studies were performed for all the synthesized compounds and the results showed that compound 4e showed greater affinity for anaplastic lymphoma kinase (ALK) receptor.
Purpose
Bioprinting is a promising technology, which has gained a recent attention, for application in all aspects of human life and has specific advantages in different areas of medicines, ...especially in ophthalmology. The three-dimensional (3D) printing tools have been widely used in different applications, from surgical planning procedures to 3D models for certain highly delicate organs (such as: eye and heart). The purpose of this paper is to review the dedicated research efforts that so far have been made to highlight applications of 3D printing in the field of ophthalmology.
Design/methodology/approach
In this paper, the state-of-the-art review has been summarized for bioprinters, biomaterials and methodologies adopted to cure eye diseases. This paper starts with fundamental discussions and gradually leads toward the summary and future trends by covering almost all the research insights. For better understanding of the readers, various tables and figures have also been incorporated.
Findings
The usages of bioprinted surgical models have shown to be helpful in shortening the time of operation and decreasing the risk of donor, and hence, it could boost certain surgical effects. This demonstrates the wide use of bioprinting to design more precise biological research models for research in broader range of applications such as in generating blood vessels and cardiac tissue. Although bioprinting has not created a significant impact in ophthalmology, in recent times, these technologies could be helpful in treating several ocular disorders in the near future.
Originality/value
This review work emphasizes the understanding of 3D printing technologies, in the light of which these can be applied in ophthalmology to achieve successful treatment of eye diseases.
An efficient synthesis of 3-substituted indoles by a sequential approach involving gold(I) chloride catalyzed cycloisomerization/bis-addition and conjugate addition of 2-(alkynyl)anilines has been ...accomplished. A variety of 2-(alkynyl)anilines, aldehydes, isatins and nitroolefins undergo this overall process in good to excellent yields. This methodology represents an effective alternative to the classical C3-functionalization of indoles.
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Alkylation of indoles has been achieved via Pd-catalyzed aliphatic C–H bond activation of tertiary amine coupling with indole followed by C–N bond cleavage and subsequent addition of indole. This ...method involves the migration of alkane chain from tertiary amine to indole.
