Design and synthesis of new Nilutamide-1,2,3-triazole derivatives as in vitro Anticancer agents

Design and synthesis of new Nilutamide-1,2,3-triazole derivatives as in vitro Anticancer agents

The synthesis of novel 1,2,3-triazoles of Nilutamide (4a–4n) via Cu(I)-promoted 1,3-dipolar cycloaddition reaction between several terminal alkynes and 1-(3-azidopropyl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione have been reported herein. In vitro anticancer activity studies of these synthesized compounds over two human prostate cell lines PC3 and DU-145 revealed that the compounds 4c, 4f and 4n exhibit slightly greater activity against two cell lines than the standard etoposide. Predominantly, the compound 4f displayed excellent activity over PC3 and DU-145 having IC50 values of 1.84and 1.34 μM respectively. The three most potent compounds 4c, 4f and 4n were also investigated for their inhibitory potential against tyrosine kinase EGFR and found that compound 4f showed superior activity than the standard erlotinib, while remaining two compounds 4c and 4n showed comparable activity with the standard.

URN:NBN:sciencein.cbl.2022.v9.405

Design and synthesis of new Nilutamide-1,2,3-triazole derivatives as in vitro Anticancer agents – https://pubs.thesciencein.org/journal/index.php/cbl/article/view/405

Chemical Biology Letters

Design, synthesis and molecular docking studies of new Quinoxaline-linked-1,2,4-triazole-Sulfonamide hybrids as Anti-proliferative agents

Design, synthesis and molecular docking studies of new Quinoxaline-linked-1,2,4-triazole-Sulfonamide hybrids as Anti-proliferative agents

A new series of quinoxaline linked 1,2,4-triazole sulfonamide  derivatives were designed and efficiently synthesized. All compounds were characterized by their IR, 1HNMR, 13CNMR, and Mass spectral data, and elemental analysis. The final compounds (5a-m) were screened for in vitro anti-proliferative activity against cancer cell lines HeLa (lung), A549 (carcinoma), MCF-7 (breast) and HCT116 (colon).The  results revealed that the compounds 5k, 5l and 5d have shown promising activity as compared to etoposide. Predominantly, the compound 5k displayed greater activity on HeLa, A549, MCF-7and HCT116 with IC50 values of 1.97±0.09, 1.84±0.07, 3.10±0.04and 4.10±0.07 than the standard drug etoposide. Moreover, molecular docking studies of 5k, 5l and 5d on EGFR receptor suggested that the most potent compound 5k strongly binds to protein EGFR (pdbid: 4HJO). Furthermore, the compounds 5k and 5l displayed promising inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.

Design, synthesis and molecular docking studies of new Quinoxaline-linked-1,2,4-triazole-Sulfonamide hybrids as Anti-proliferative agents – https://pubs.thesciencein.org/journal/index.php/cbl/article/view/396

Chemical Biology Letters

Content composition is key for good citations

The researchers publishing their work and thinking ‘How do I get more citations to my article?’ or want to ensure good citations to their work, then they should work on the contents for proper presentation before publication.

Content is the Key

You should work to produce a good quality, content rich article (research or review article). Quality of your work is the main criteria that researchers will like to refer to your article.

Composition

The title, authors, affiliations, abstract, keywords are the front page of your article, that are circulated in all the databases and search engines. The proper composition of these elements can bring more readership and more citations to your article.

You should work on these before final publication of your article.

Title

The title of your article should be comprehensive, clear, and precise that reflect the contents of your article. Try to avoid question marked titles (it is observed that such articles have more readers/download, but cited less).

Authors

Each author of article should ensure that he/she is using a consistent name in their publications. (In Indian context, female scholars should choose a name and surname such a way that they can use that before the marriage and after the marriage as well. Changing the surname particularly after marriage create problem in indexing/identification of that properly). It is good to include a ‘surname’ or family name in their name. This will help to identify the respective researcher correctly and associate their work. Few authors have lengthy names or very short name (either multiple words names or one word names), they should identify clearly their first name and last name (surname) properly. It is good to have clear 2 or 3 words name (first name and last name). Using the same name on all of your papers will make it easier for others to find all of your published work

Affiliation

The name of your institution should be written properly and in uniform format.

Abstract

Your abstract of article should be containing the details of contents of your article, and importantly should have phrases, and keyword that a reader might use to search your article. The keywords and phrases may be repeated in title and abstract. Inclusion of selected search related phrases in abstract increases the chances of listing your article in top result in search engines (google etc.) which increases the likelihood of reading your article and thus citation of your article.

Keywords

You should carefully select the keyword for your article. Choose such keyword that any reader might use for searching the contents of your article in search engines (google etc.). While compiling your article, you might have used few keyword in search engines to search the related works, same/similar keywords may listed in your article so that other researchers can find your article easily. So choose your keyword carefully. The keywords are meant for finding your articles with these general keywords in google search.

Post publication

Once your article is published, then you should work to promote and get cited your article. See the tricks that you can use to get more citations to your work.

Citations to published articles – 15 relevant methods for improving profile of authors

The citations to the published works indicate the relevance of specific piece of work (research article, review article, short communication etc.) for research community. The citations to articles enrich the profiles of authors and are beneficial for ranking of the institutes/universities.

Citations to published articles are directly relevant for Authors’ profile and Institution Ranking..

In the current scenario of publish and popularize, the authors/researchers should take steps to inform the research community about their new published work/article (simply indexing in databases is not sufficient). You may refer to Prof. Jeff Ollerton blog to understand ‘why you should promote your work’ at https://jeffollerton.co.uk/2015/01/08/what-do-academics-do-once-the-research-is-published/  

You need to promote your work (Popularize), no one else will do it for you.

There have been many research advances to understand the different aspects and methods that brings increased citations to a published article (see references below). Herein are listed the prominent methods which on systematic adoption will bring more citations for authors

Best methods to improve your citations counts – check list below:

Concise compilation of article:

  1. The title, abstract and keywords of the article should be containing the relevant details which can list your article on the top in search result in any online search engine (google, bing, yahoo etc.). refer to ‘content composition’ hints for your article.

Share on your webpage

  1. Make your professional webpage and list your article on your webpage. Preferably, the webpage should be on your institute/university website, if not then develop your own. Self-archiving of your article on your webpage makes it easily searchable and bring more citations. Always insert link to the original source (journal site) to the list of your articles (authenticity of work give researchers a reason to cite repeatedly).

Publish your work with Open Access

  1. Open access of your article brings more citations. It has been reported by many researchers and have recently been observed that the articles published with ‘open access’ gets more citations. So, preferably publish your work with open access.

Publish in collaboration

  1. Collaborate and publish your work with international authors. This is another value addition factor to your article,
    (a) collaborative publishing with international authors indicates an inclusiveness of diversity and gives a better chance of getting cited by researchers from different countries (by authors itself as well as readers).
    (b) Team authored articles gets more citations (it is good to collaborate and have more authors on your article). The multiple authors provide multiple opportunities for promoting the work, and also they are more likely to cite the work.
    (c) Publishing with senior researchers (or Noble laureates) brings authenticity as well as citations to your article.

Collaborative publishing is the key for higher citations.

Collaborative team publication are always on better side for total count of citations.

Publish a review

  1. Publish a detailed lengthy paper with inclusion of more references. It has been reported by researchers that a lengthy article and articles with more references generally gets more citations. Review paper gets more citations.

Blog your work

  1. Start blogging about your published work. Write and post a small paragraph giving the general importance of your work in a layman language (so every one can understand your work), include link to your article on journal site in your blog so that readers can easily find your article.

Social Share

  1. Share on Academic and Networking site. You inform your close colleagues about your work when you share link of your work on social networking site (LinkedIn, Researchgate, facebook, academica etc.).

Insert ‘callout’

  1. Include a ‘callout’ in your article as papers with ‘callout’ gets more citations. Callout are general interpretation of discussion and readers quickly gets your message/interpretation which increases the chances of getting cited your article.

Include article in Email Signatures

  1. Include your recent article title and link in your Email Signature. Your email readers (mostly your colleague and network) will notice your work via this method and will cite your article.

Share Data

  1. Always share your experimental data (as supplementary file or on as result dataset on any archival sites). Works with complete details are referred more by researchers and gets upto 60% more citations.

Present in conferences

  1. Share your article in conference presentations, your targeted audience get noticed of your work in field specific conferences. Include your article details/citation in your presentation.

Share podcast of your work

  1. Create a podcast / video of your work and share it on youtube or vimeo, link to original article should be inserted in description of video podcast. Visual / video makes the reach to more researchers, would bring citations to your work.
Share on different text sites
  1. Share your article on wiki sites (Wikipedia) and other similar sites. Sharing on different sites will bring your article in very results on google search and other search engine; creating more readership and more citations.
Deposit in institutional repository
  1. Deposit your article or abstract on your institutional site or repository. Scholars from your institute search the local repository and find your article.
Cite
  1. Cite your article / past work when it is relevant to your current work/article. (do not cite unrelated articles).     

Start adopting each of above points, let us know your results. Did you get any improvement in your citation count, and author profile then share your thought to us.

(Any additional suggestion in above list or correction/update are also welcome, write to us using contact us page).

Additional readings:

https://mpra.ub.uni-muenchen.de/50919/1/MPRA_paper_50919.pdf

Medicinal active applications of Dibenzofuran derivatives

Dibenzofuran is an important heterocyclic compound and is an important part of various natural compounds. There are various medicinal compounds containing dibenzofurans, sold in the market to combat different human diseases and plant infections. Research on dibenzofuran is an advancing field in the medicinal science. Several compounds are under the clinical trials and are expected to be utilized in various treatments. This review article encompasses various advancements in the study of these dibenzo derivatives. The biological activity of these scaffolds hovering around cytotoxicity of the cells, bacterial infections, fungal infections, type-2 diabetes, platelet coagulation and in the effective skin treatment, has been discussed in the following article.  The toxicology of the compound is also argued and selected biological applications are hereby discussed to make easier for the researchers to have a consolidated sight over the topic.

Linkhttps://pubs.thesciencein.org/journal/index.php/cbl/article/view/374
published in Chemical Biology Letters

Investigation of molecular interaction between β-amyloid and insulin receptor: An in-silico study

The growth of amyloid β peptides arises from inappropriate cleavage of amyloid precursor protein that induces the formation of amyloid plaques in the brain. An excessive accumulation of amyloid β plaques promotes the development of dementia, specifically Alzheimer’s disease (AD). Histopathological evidence suggested that insulin resistance and type 2 diabetes condition have a stronger correlation with Alzheimer’s disease development. An increasing concentration of amyloid β leads to impaired binding of insulin to its receptor. Previous studies suggested that the monomeric form of amyloid β was the potential molecule, which can compete with insulin for receptor binding. The objective of this work was to study the molecular interactions of insulin and amyloid β to insulin receptors using protein-protein docking and molecular dynamics Simulations. Analysis of docked complexes suggested that there are common insulin receptor residues for insulin and amyloid β binding. Further molecular dynamics Simulations study reveals that the monomeric form of amyloid β interacts with a similar set of receptor residues as observed in the insulin-insulin receptor complex.

Author Guidelines for Journal of Integrated Science and Technology

The Authors need to submit a single manuscript file containing all the figures/tables/graphs/othergraphics and text as described below. The supplementary data files should be submitted as a separate file. Authors are advised to prepare their manuscript according to journal article template provided below.

Cover letter

Authors should supply a cover letter indicating rational of their work. Cover letter should also have details of at least three reviewers (with email). Cover letter should be provided on the first step of submission in “Comments for Editor’ box.

Graphical Abstract

Authors need to submit a graphical abstract highlighting the contents of manuscript. Graphical abstract could be submitted as supplementary file or on the last page of manuscript. The preferred image size of graphical abstract is 700px x 250px

Manuscript

Manuscript should include Title, Author (s), Affiliation (complete name of institutions), Abstract, 5 Keywords, (other sections like Introduction, Results and discussion, conclusion, experimental procedures in the main body text of manuscript could be used for full paper article), acknowledgment and references in the listed order. Short communications need not to be arranged in different sections. References should be formatted as shown for articles,1 theses,2 books,3,4 and patents,5

1. R. Ping, M. Laura, P.S. Mario. Title of the journal article should be included here. Int. Lett.Org. Chem. 1996, 61, 4439–4449.
2. B.K. Sharma. Ph.D. Dissertation, Thesis Title, Cornell University, 1995.
3. R. Hussain, D. Shinkoi. Title of book like Synthesis and application of ionic liquid, John Wiley & Sons: New York, 2010.
4. R.S. Buchanod, D.K. Reddy. In Selective Organic Transformations; T.R. Thyagarajan, Ed.; Integrated science: New York, 2002; Vol. 2, pp 1–95.
5. G.L. Loyale, U.S. Patent 5 934 456, 1998; Chem. Abstr. 1998, 65, 2870.

Citation Manager style files: Authors are highly encouraged to use the citation manager programs for citing and formatting the references. Authors may use Mendelay, Zotero, Paper 2 or Endnote program. If you are using any of these citation manager program for Bibliography (References and Notes), then you can download citation style file for journal (common for all ScienceIn journals):

Mendelay, Zotero, Paper 2 style file: ScienceIn Journals CSL style file

Authors can directly add the styles to Zotero and Mendeley, follow the below steps:
Zotero: Open Zotero desktop > Edit (top menu)> Preferences > Cite (menu in new opened small window) > Get additional styles.. (click this link below the list of styles) > in new opened window – search the term ‘Integrated Science’ in search box and then click on ‘Integrated Science Publishing Journals’ link > style file will download > Open the file with Zotero desktop and use (this style is common for all ScienceIn Journals).
Mendeley: Open Mendeley desktop > View (top menu) > Citation Styles > More styles.. > go to tab ‘Get more styles’ (in new opened window) > search for the term ‘Integrated Science’ in search box and then click on ‘install’ adjacent to ‘Integrated Science Publishing Journals’ list > style file will be installed > then click on ‘Use this style’ from the installed styles tab and use (this style is common for all ScienceIn Journals).

Endnote style file: ScienceIn Journals Endnote style file

(click and download the endnote style file from google drive … and either copy the file to Endnote style folder (go to C:>Program files>Endnote > Style folder > paste the file in this folder (it will listed in style when you open the Endnote program) or you can directly Open the downloaded style file in EndNote program and use).

Also the user can check the respective program user guide (online link on Zotero, Mendeley or Endnote) regarding information on how to use the style file.

On acceptance of manuscript, authors must need to supply their manuscript in Article template (if they have not already submitted in template).

Submission

Authors need to submit all manuscripts through journal website. Register by following link ‘Register’ above (make sure to mark checked the options Author and reviewer while registering for journal). On login, you will find ‘new submission’ link in your panel page.

Templates

On acceptance of manuscript, Authors are required to submit revised manuscript in journal articles template (If authors wish, they are free to submit their manuscript in journal article template while submitting first time).

download from the link

download the template, double click the file to open and then prepare your article and save it with your own name.

Instructions for conversion of manuscript in journal article template is provided on https://pubs.thesciencein.org/manuscript-conversion-in-journal-article-template-instructions/  (please check the video on the link for correctly formatting your manuscript.

Submission:

Login and submit the manuscript online (submission by email are not accepted). Only online submissions are accepted now.

https://pubs.thesciencein.org/journal/index.php/jist

Lipid based self-assembled nanostructures for therapeutic delivery applications

The evolution of lipid nanoparticles (LNPs) has been remarkably interesting and in beneficent directions for food and health industries working towards human well being. Since the discovery of the first-generation lipid based self-assembled nanostructures, i.e., liposomes in the 1960s, it has witnessed significant advances in their development and distinctive potential in different application domains. Based on the composition and structure, these lipid based structures have varied from liposome to lipid nanoparticles such as nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLN) to overcome certain limitation pertaining to their use in different fields. The outstanding application of LNPs as therapeutic delivery systems has made them key players to treat different human disorders including the fatal cancers. Their life-saving global contribution has recently been witnessed in the form of mRNA vaccines against deadly COVID-19. They have also significantly served purpose in other domains such as biomedical imaging, cosmetics, nutrition, and agriculture. Their prominent role is in the area of anticancer therapy as delivery vectors for nucleic acids and drugs. Some issues with respect to the cellular delivery of drugs and genes, such as circulation time and stability have been somewhat resolved, but the unmet goal of site-specific substantial delivery remains the main focus in LNPs development research. Despite the promise shown by LNPs in animal studies and the fact that technological advances in LNPs research have made the approval possible of a few formulations, therapeutic outcomes in human are not satisfactory. The LNPs technology has managed to survive due to possible tailoring of their properties by virtue of the possibility of altering the composition and modifying the surface. Therefore, enormous scientific endeavours are on the rise to transform lipid structures, composition along with tinkering with surface of LNPs. The alternative methods to guide LNPs coupled with advances in small molecule nucleic acid therapeutics and drug development technology to make the entry possible to specific cells may be effective in cancer therapy. The development is very promising; however enduring efforts are required till the goal is reached.

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/368

Published in : Chemical Biology Letters

Impact of Ayurvedic drug Tinospora cordifolia in hyperlipidemia induced dysbiosis

Gut microbiota broadly impacts human health, but urinary microbial metabolites remain largely undefined. The concentration of microbial metabolites can be directly correlated with microbial populations in the human gut to define disease states. Tinospora cordifolia (Willd.) Miers ex Hook. F. & Thoms is being used for ages in the Indian ayurvedic system of medicine and it has hypolipidemic and hypoglycaemic activity. Present study investigate the MS-based metabolomics variations of possible gut microbiota associated metabolites in hyperlipidemia (HPL) and HPL treated with Tinospora cordifolia extract (TCE) (TRT). Twenty-four HPL male patients and 10 age-matched controls (HLT) were enrolled. Early morning fasting blood and urine samples were collected on days 0 and 14th of TCE treatment and subjected to lipid profiling and Q-TOF-MS analysis. Multivariate analysis showed urinary levels of urocanic acid, hydroxyphenylacetate, linolenic acid, phenylpropionate, hypoxanthine, and indole acetate produced by Peptostreptococcs asaccharolyticus, Clostridium difficile, Faecalibacterium prausnitzii, Bifidobacterium, Subdoligranulum, Lactobacillus, Clostridium sporogenes, E. coli were depleted in HPL patients as compared to healthy controls. In contrast, levels of serotonin, acetylleucine, hippuric acid, and arabinitol were found to be increased (>2.0 fold, p<0.005). However, TCE treatment reverted the levels of these metabolites and therefore, gut microflora. Also, Cloacibacterium haliotis, Lactobacillus, Clostridium, and Bifidobacterium population decreased in HPL patients. Increased secretion of yeast or Candida albicans associated metabolites was because of their increased population. Hence, TCE treatment enhanced the growth of useful gut microbiota in hyperlipidemia patients.

Linkhttps://pubs.thesciencein.org/journal/index.php/cbl/article/view/363

Chemical Biology Letters

Gas sensing of partially oxidized Ti3C2Tx MXene in argon atmosphere

Multilayer accordion like Ti3C2Tx MXene is prepared by selective etching of Al layer from Ti3AlC2 MAX phase.  For better gas sensing responses, a minimal amount of TiO2 decoration is being carried out by annealing the Ti3C2Tx MXene in an argon atmosphere at 550 °C for 6 h. The X-ray diffraction pattern shows successful removal of Al layer and TiO2 decoration on Ti3C2Tx MXene surface which is well supported by field emission scanning electron microscope images. Due to TiO2 decoration, MXene shows semiconducting behaviour and corresponding bandgap is 3.2 eV. Resistance of TiO2 decorated MXene sample increases in presence of H2, CH4 and NO2 gases at room temperature. However, resistance of the sample decreases for H2, and CH4 gases and increases for NO2 gas at 100 °C which shows n-type semiconducting behaviour. Also, at 100 °C, sensitivity increases by one order to that of room temperature gas response of TiO2 decorated MXene sample.