Synthesis and biological evaluation of Trifluoromethoxyphenyl Indole Carboxamide analogs, ADME and toxicity prediction
We report synthesis, ADME profile, and biological evaluation of new analogues as effective Anticancer Agents. Trifluoromethoxyphenyl indole-5-carboxamide analogues (4a-4m) were developed as a class of strong inhibitors of BCR-ABL1 kinase. The compounds (4c, 4e, and 4m) showed good anticancer activity in cancer cell lines such as MCF7, MV411 and K562 with IC50 values of 1.4 µM, 1.7 µM, and 1.1 µM, respectively. In human liver microsomes, these substances likewise displayed a favorable ADME profile, good solubility, and minimal clearance. In an oncology program these analogues offer a promising beginning for the development of BCR-ABL1 kinase inhibitors.
Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment
Mitogen-activated protein kinases (MAPKs), also known as extracellular signal regulated kinases (ERKs), are found in numerous signal transduction pathways and are triggered by protein kinase cascades. This article will review the present state of MAPK pathway inhibitors, with an emphasis on the characteristics of tiny molecule blockers of the p38, MEK1, and MEK2 protein kinases. Many of these inhibitors have showed potential in experimental animal models of disease, and they are now being investigated in people for inflammatory and cancer diseases. Clinical trials are currently evaluating targeting a subset of cellular signaling cascades and signaling cascades that control pleiotropic cellular activity. These activities will have far-reaching consequences for the management of a wide range of disorders. The Ras-Raf-MEK-ERK (ERK) pathway, on the other hand, is a clear therapeutic target because it is a common downstream route for a range of critical growth factor tyrosine kinase receptors that are frequently changed or overexpressed in human malignancies. Several new medicines that target this route have been discovered and are currently being tested in clinical studies. BAY 43-9006 is one of the most intriguing new agents. Although it was initially created as a Raf kinase inhibitor, it also has the ability to target Flt-3, c-Kit, and VEGFR-2, which helps to explain its antiproliferative and antiangiogenic characteristics. The ERK signaling system in normal and malignant tissue will be discussed in this paper, with a focus on emerging treatments that target the ERK cascade at the Raf kinase level.
Remodeling of membrane lipid homeostasis in azole resistant isolates of Candida albicans
Azole resistance mechanisms in Candida albicans infections majorly focus around the alteration of target enzymes, overexpression of efflux pump proteins, and changes in lipid metabolism. Our earlier lipidomic studies have linked changes in cellular lipid compositions to drug susceptibilities and phenotypic defects. This study investigates the relationship between whole cell and membrane lipid profiles in isogenic drug-susceptible and resistant isolates of C. albicans. We have examined the fatty acid and sterol snapshot lipidomics in whole cells, plasma membrane, and lipid rafts. Correlations were discovered between these lipid compositions and the observed drug resistance in C. albicans. Although the correlations drawn from cellular and plasma membrane data corroborate, understanding plasma membrane and suborganellar (rafts in this case) lipid changes may provide better insights into their roles in efflux pump activities and localization, and drug susceptibilities.
The ScienceIN offers fellowship to support the scholars for attending the national and international science conferences and symposium in India. The ‘Conference Fellowship’ from The ScienceIN covers the full registration fee of participants (preferably young researchers – Ph.D. students, Research Associates, PDFs, and young faculty/scientists) via either waive off (for future sponsored conferences) or refund (already completed conferences).
Conference fellowship for 2024
At present 50 Conference Fellowships are available for the participants of the
CRSI – National Symposium in Chemistry – 32 held at BITS Pilani, Pilani 2-4 Feb 2024.
The participants of the CRSI-NSC-32 can claim the refund of their registration fee (full – excluding other fee, if any) if they have published any article in JMC or ML (or can publish an article in JMC or ML before the last date (i.e. 31-Oct-24) for claim). – Submit your registration fee slip (snap or online transfer details) and title of published article (JMC/ML) to the pubs@thesciencein.org for refund. – Provide the bank details/upi id for online refund of your registration fee (the fellowship will be directly credited in Scholar’s account). – One author from respective article will be eligible for refund. – Articles published or accepted for publication before the last date of claim (31-Oct-2024) will be eligible of this fellowship. – First come first served will be the process for disbursing the fellowships. – It is for Indian Scholars only (fellowship in INR will be credited).
————-
All future announcements related to Conference fellowships will be on this page, scholars can visit this page for open fellowships for attending the science conference.
> The Authors need to submit a single manuscript file containing all figures and tables. > The supplementary data files should be submitted as a separate file. > A cover letter and graphical abstract should be submitted along with manuscript as details 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.
Manuscript should include Title, Author (s), Affiliation (complete name of institutions), Abstract, 5 Keywords (refer https://pubs.thesciencein.org/content-composition for details), (other sections like Introduction, Results and discussion, experimental procedures, conclusion 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):
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).
(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.
Submission
Authors need to submit all manuscripts through journal website. Register by following link ‘Register’ on the journal site https://pubs.thesciencein.org/journal/index.php/btl (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.
For review purpose, author can submit the manuscript as outlined above. However, Authors are advised to prepare their manuscript according to journal article template (provided below) as it progress towards acceptance. On acceptance of manuscript, authors must need to supply their manuscript in Article template (if they have not already submitted in template).
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).
Login and submit the manuscript online (submission by email are not accepted). Only online submissions are accepted now.
Authors are advised to contact Support, BTL (email: pubs @ thesciencein.org ) if there is any problem in registration or submission.
Unique IDs for Articles: The journal is currently using URN number for the published articles (however, this is currently meant for internal use by journal). The journal will process the assigning of DOI (Digital Object Identifier) to articles from 2024 vol. 11 issue 2 onwards.
Declaration of Conflict of Interest
Authors should mention any conflict of interest in the work submitted to Biomedical and Therapeutics Letters. The statement about conflict of interest may be mentioned in the ‘Letter to editor’ and placed in the manuscript after acknowledgement section.
Authors need to check the details of ‘Conflict of Interest’ for authors of scientific works.
Ethical Uses Declaration
If the manuscript report the experimentation on animals (including clinical trials on human beings), then declaration about ethical way handling of animals and about keeping the complete privacy of human identity (in case of clinical trials) must be mentioned in the manuscript.
Helsinki Declaration (contents from NIH-NLM): When reporting experiments on human subjects, authors should indicate whether the procedures followed were in accordance with the ethical standards of the responsible committee on human experimentation (institutional and national) and with the Helsinki Declaration of 1975, as revised in 2000 (5). If doubt exists whether the research was conducted in accordance with the Helsinki Declaration, the authors must explain the rationale for their approach, and demonstrate that the institutional review body explicitly approved the doubtful aspects of the study. When reporting experiments on animals, authors should be asked to indicate whether the institutional and national guide for the care and use of laboratory animals was followed. See the detailed instructions on https://www.wma.net/policies-post/wma-declaration-of-helsinki-ethical-principles-for-medical-research-involving-human-subjects/ and https://www.wma.net/policy/current-policies/ (for recent applicable policy documents).
Authors need to check and follow the general Ethical Practices for Authors of scientific work.
Submission Journal Link
Submit manuscript on journal editorial processing site at
The SGVU – Biotechnology Business Incubator and School of Applied Sciences, Suresh Gyan Vihar University (SGVU), Jaipur, India is organizing an International Conference on BIOTECH NEXUS-2024- “Recent Advances in Biotechnology and Biomedical Sciences” on 26th- 27th April 2024. The conference aims at bringing together scientists working in the field of cutting-edge biotechnology and biomedical sciences to discuss groundbreaking advancements that have the potential to address urgent demands of healthcare and agriculture. The conference will serve as avenue for promoting global network among expert scientists and industry personnel to showcase the research developments. The event provides the opportunity to researchers at various levels for showcasing recent developments and ideas to overcome bottlenecks towards improved health and environment.
The breakthroughs in biotechnology and nanobiotechnology are playing a crucial role in improving the healthcare services for modifying treatment procedures and enhancing patient outcomes. The products of biotechnology have been significantly commercialized while providing promising solutions to biotechnology bottlenecks. In contrast, biotechnology has remarkably influenced the field of agriculture while managing crop production relating to food and medicine. On the other hand, continued advancements in biomedical sciences have been underpinning the with a great hope for successful treatments of different human health disorders.
This special issue will cover the recent developments in research pertaining to the development of new natural and synthetic drug candidates, innovative therapeutic delivery systems and methods, nano-/biomaterials and their application, novel biosensors, biomolecule detection technologies and biomedical devices, studying molecular and cellular mechanisms in stem cell and cancer research, studying immune system function and development and immunotherapeutic approaches, progress in Computational biology and bioinformatics, diverse tools for environmental remediation and environmental toxicology, tools and technologies in agricultural sciences and AI applications in health care.
Themes of special issue
Natural/synthetic Products in drug discovery and design
Innovative drug/Gene delivery systems in non-communicable disorders
Nano-/Biomaterials, Biosensors and Biomedical devices
Stem cell and cancer research biology
Immunobiology and cell biology
Molecular Dynamics, Structural Biology and Bioinformatics
Environmental Remediation and Toxicology
Sustainable Agribiotech Solutions
Artificial Intelligence/Machine Learning and OMICS
Guest Editors
Prof. (Dr.) Gaurav Sharma Professor and Principal School of Applied Sciences Suresh Gyan Vihar University Jaipur, India
Dr. Neha Kapoor Associate Professor School of Applied Sciences Suresh Gyan Vihar University Jaipur, India
Dr. Krishan Kumar Associate Professor School of Applied Sciences Suresh Gyan Vihar University Jaipur, India
Pervasive computing, also known as ubiquitous computing, refers to the integration of computational capabilities into everyday objects and environments, enabling seamless interaction between people and technology. This concept envisions a world where computing devices are embedded in various forms – ranging from household items and wearable gadgets to urban infrastructure – creating an interconnected environment that enhances the efficiency, convenience, and intelligence of our daily activities. By making technology invisible and intuitive, pervasive computing aims to create a user experience that is both immersive and natural, allowing individuals to interact with digital systems without being consciously aware of the underlying technology. As it continues to evolve, pervasive computing holds the potential to transform industries, improve quality of life, and redefine how we engage with the world around us.
This special issue is meant to cover the research in Pervasive computing focusing on the following sub-disciplines:
Signal and Image Processing
Embedded System and VLSI Design
Soft Computing and Computer Vision
Big Data and Cloud Computing
Internet of Things
Wireless Communication System
Network and Information Security
Electric and Hybrid Vehicles
Power Electronics and Electronic Devices
Robotics and Autonomous Vehicles
Block Chain and Distributed Ledger Security
Industrial Automation
Multidisciplinary Aspects of Engineering
Guest Editors
Dr. Supriya O. Rajankar Professor Electronics and Telecommunication Department Sinhgad College of Engineering, Pune. India
Dr. Omprakash S. Rajankar Professor Electronics and Telecommunication Department Dhole Patil College of Engineering, Pune. India
Dr. Vrushali G. Rout Associate Professor Electronics and Telecommunication Department Sinhgad College of Engineering, Pune. India
Invitation
Scholars working in the field are invited to submit their work for consideration in the special issue. The participant of the National Conference on Pervasive Computing (NCPC)-2024 (April 05, 2024 ) Organized by Department of Electronics and Telecommunication Engineering, Sinhgad College of Engineering, Pune, India are encouraged to submit their work for consideration. All submissions will undergo peer-review and only articles recommended by independent reviewers will be considered for publication processing.
Submissions
(closed – Issue has been published, see link below) Authors need to submit their work to the guest editors for preliminary screening, and approved articles need to be submitted on journal site.
Design, synthesis and biological evaluation of novel sulfamoyl benzamides as allosteric activators of human glucokinase
Glucokinase (GK) activators, which target the GK enzyme, are an emerging class of therapeutics with promising effects against diabetes. The objective of this work was to create a new group of sulfamoyl benzamide derivatives with the ability to activate GK and evaluate their effectiveness in treating diabetes. From benzoic acid, several compounds containing sulfamoyl benzamide scaffold were synthesized and evaluated for their ability to activate GK in an in vitro enzymatic experiment. In silico docking analyses were employed to explore how the most suitable arrangements in the allosteric area of the GK enzyme interact during binding. The effectiveness of the identified substances in reducing high blood sugar levels was assessed using the oral glucose tolerance test (OGTT) in healthy rats. This evaluation was based on the results of laboratory tests on enzymes and in silico simulations. One of the most active compounds from the antihyperglycemic assay was then tested for its antidiabetic effects in an induced diabetic rat OGTT assay. The in vitro GK activation was best among compounds 1, 6, and 8 (activation fold: 2.03-2.09). In the OGTT assay (normal rats), compounds 1 and 6 showed promising antihyperglycemic activity. In vivo antidiabetic assay confirmed the consistency with in silico and in vitro outcomes. The newly synthesized derivatives of sulfamoyl benzamide have the potential to be used as a basis for the development of further GK activators that are both safe and efficacious and can be administered orally. These activators may be used as therapeutic agents to treat type 2 diabetes.
Molecular pathways with role to play in oral cancer: A mini-review
Oral cancer is the sixth most prevalent type of cancer worldwide and third in India out of the different cancer types identified. Mouth and oral cancers collectively refer to cancers of the buccal cavity, lips, oropharynx, hypopharynx, and larynx. Genetic anomalies, the upregulation of several proteins, the deregulation of tumor-suppressive and oncogenes, and risk factors like alcohol and tobacco consumption are a few examples of the known irregularities that contribute to the development of oral cancer through the accumulation of various carcinogenic substances. Oral cancer is caused and developed by multiple molecular and cellular pathways such as PI3K/AKT/mTOR, Ras-Raf-MEK-ERK pathway, Wnt signaling, NF-κB pathway, Hippo pathway, etc. In addition, various genes including TP53, PTEN, CDKN2A, HRAS, PIK3CA, NOTCH1, IRF6, TP63, etc. are also involved in this malignancy. Therefore, it is crucial to have a deep understanding of these pathways to properly understand the development of oral cancer. This short review focuses on compiling together various signaling and molecular pathways accountable for oral carcinoma development.
Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents
The synthesis of new indole-oxadiazole coupled isoxazole hybrids (6a–o) synthesized by the Cu(I)-catalyzed reaction of in situ generated nitrile oxides with 3-(3,5-dichloro-4-methoxyphenyl)-5-(1-(prop-2-yn-1-yl)-1H-indol-3-yl)-1,2,4-oxadiazole in good yields have been reported here. The chemical structures of all newly synthesized hybrids were confirmed by 1H-NMR, 13C-NMR, and Mass spectra. All synthesized compounds were screened for their in vitro cytotoxicity against two breast cancer cell lines MCF-7 and MDA-MB-231 respectively. All the derivatives were more active against MCF7 than MDA-MB-231 cancer cells and few compounds showed better activity than the standard erlotinib. The ability of more potent compounds to inhibit EGFR tyrosine kinase, one of the key enzymes involved in breast carcinomas was evaluated by in vitro enzymatic assay and it was found that the compound (6g) and (6m) had more inhibitory activity IC50 values 0.311±0.05 and 0.203±0.03 mM than erlotinib (IC50=0.421±0.03 mM).
