Updates

Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3

urn:nbn:sciencein.cbl.2019v6.113

Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3

Published in Chemical Biology Letters

  • Pooja FNU University of Delhi
  • Nimisha Sinha University of Delhi
  • Sonu Kumar University of Delhi
  • Atul FNU University of Delhi
  • Sumit Kumar University of Delhi
  • Prashant Kumar SRM University
  • Abhishek Pandey University of Delhi
  • Pragya Sharma University of Delhi
  • Vithika Aggarwal University of Delhi
  • Poonam FNU University of Delhi
  • Poonam Mothsra University of Delhi
  • Brajendra Kumar Singh University of Delhi
  • Rishi Pal Singh University of Delhi
  • Yogesh Kumar University of Delhi

Keywords: Apoptotic inducer activity, anti-cancer, anti-tumor, breast cancer, enzyme inhibition, medicinal chemistry

Abstract

Coumarin, triazoles and thiazolidinones are one of the most preferred and high valued scaffolds frequently used in medicinal chemistry. The synthesis of newly designed coumarin based triazolyl-thiazolidinones was performed and new compounds were obtained in good yields. The listed compounds were evaluated for their apoptotic activity and determined the minimal inhibitory concentrations for each of the compound on SCC-4 cells using MTT viability test. Furthermore, apoptotic inducer activity was assayed by detecting the expression of caspase-3, a key apoptotic enzyme.

Cite as: FNU, P., Sinha, N., Kumar, S., FNU, A., Kumar, S., Kumar, P., Pandey, A., Sharma, P., Aggarwal, V., FNU, P., Mothsra, P., Singh, B., Singh, R., & Kumar, Y. (2019). Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3. Chemical Biology Letters, 6(2), 30-38.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/113

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

urn:nbn:sciencein.cbl.2019v6.111

Published in Chemical Biology Letters

  • Deepak Mishra Delhi Technological University
  • Atiya Fatima Delhi Technological University
  • Ram Singh Delhi Technological University
  • Nupur S Munjal Jaypee University of Information Technology
  • Vineet Mehta Jaypee University of Information Technology
  • Udayabanu Malairaman Jaypee University of Information Technology

Keywords: Alzheimer’s Disease, Brain disease, medicinal chemistry, coumarin derivative, AChE, BuChE, Nervous system, Neurological

Abstract

In this paper, we report the design, synthesis, in-silico, and in-vitro evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives have been synthesized separately, and further combined through covalent amine bond linkage. The synthesized compounds showed more inhibition towards BuChE than AChE, where 4-(3-bromophenyl)-1,3-thiazol-2-amine (7i) exhibited the strongest inhibition against BuChE with an IC50 value of 3.54 μM. For the conjugates, 3-{2-[4-(3-nitrophenyl)thiazol-2-ylamino]acetyl}chromen-2-one (8j) exhibited strongest inhibition with an IC50 value of 46.47 μM.  The better inhibition activities towards BuChE are also shown by 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole moiety produced better results against BuChE than 4-substituted counterparts.

Cite as: Mishra, D., Fatima, A., Singh, R., Munjal, N., Mehta, V., & Malairaman, U. (2019). Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors. Chemical Biology Letters6(2), 23-30.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/111

Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays

urn:nbn:sciencein.jmns.2019v6.109

Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays

Published in Journal of Materials NanoScience

  • Suman Sheoran M.D. University
  • Sitender Singh M.D. University
  • Ajay Mann M.D. University
  • Anura Samantilleke Universidade of Minho
  • Bernabe Mani Universitat Politecnica de Valencia
  • Devender Singh M.D. University

Keywords: nanophosphors, displays, lanthanide, luminescence, composites, LED

Abstract

A series of Eu3+ doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) was synthesized via sol-gel procedure at 950 oC. The optical characteristics of the materials were studied by Photoluminescence (PL) emission spectra. Upon 395 nm excitation and at 0.03 mole concentration of Eu3+ ion, these nanophosphors display optimum photoluminescence with most intense peak due to 5D07F2 (614-616) of dopant. Powder X-ray diffraction (PXRD) analysis proves that all synthesized materials are of crystalline nature and crystallinity improves on increasing temperature. Transmission electron microscopy (TEM) exhibited the spherical shape of particles in 13-30 nm size. Fourier Transformation infrared (FTIR) spectra showed peaks in 400-1000 cm-1 corresponding to gadolinium-oxygen and silicon-oxygen bond vibrations. In BaGd2Si3O10 material, Gd-O vibration is centered at 492 cm-1 and absorption band at 855 cm-1 is result of asymmetric vibrations of SiO in silicate tetrahedral unit. Due to excellent photoluminescence and suitable CIE coordinates, these materials could have brilliant applications in innovative displays.

Research Highlights

  • Series of trivalent europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+)fluorescent materials were synthesized successfully with sol-gel procedure.
  • The prepared samples were characterized using Photoluminescence analysis, X-ray diffraction study, Transmission Electron Microscopic analysis and Fourier Transform Infrared spectroscopy.
  • The CIE color coordinates values of phosphor confirmed the red color of complex approving the PL results.
  • X-ray diffraction pattern of these materials determined the particle size using Debye Scherrer’s equation.
  • Excellent photoluminescence response and nano size of these materials made them suitable for various innovative display applications.

Cite as: Sheoran, S., Singh, S., Mann, A., Samantilleke, A., Mani, B., & Singh, D. (2019). Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays. Journal of Materials NanoScience, 6(2), 73-81.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/109

Low-temperature microwave-assisted synthesis and antifungal activity of CoFe2O4 nanoparticles

Low-temperature microwave-assisted synthesis and antifungal activity of CoFe2O4 nanoparticles

urn:nbn:sciencein.jmns.2019v6.108

Published in Journal of Materials NanoScience

  • T. R. Ravikumar Naik Indian Institute of Science
  • Naveen Joshi Indian Institute of Science
  • S.A. Shivashankar Indian Institute of Science
  • P.J. Bindu Indian Institute of Science

Keywords: Microwave, cobalt ferrite, nanocrystalline, metal, complex

Abstract

Nanoparticle ferrite with chemical formula CoFe2O4 was prepared from the Co (II) and Fe (III) 3-acetyl-4-hydroxy-coumarin metal complexes by solution based one-pot microwave assisted technique. Single phase structure of CoFe2O4 ferrites nanoparticles was confirmed using FTIR, XRD, SEM, and EDX analysis. Transmission Electron Microscope (TEM) showed that the particle size of the samples in the range of (15 nm). The hysteresis studies showed ferromagnetic behaviour at room temperature. The antifungal activity of CoFe2O4 nanoparticle was investigated against A.flavus and A. niger by employing disc diffusion method. According to the results obtained, CoFe2O4 is a potential material for antifungal diseases. The CoFe2O4 nanoparticles could be readily separated from water solution after the disinfection process by applying an external magnetic field.

How to Cite Naik, T. R. R., Joshi, N., Shivashankar, S., & Bindu, P. (2019). Low-temperature microwave-assisted synthesis and antifungal activity of CoFe2O4 nanoparticles. Journal of Materials NanoScience, 6(2), 67-72.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/108

Drug delivery with nano-materials – significance and advances in Medicinal Chemistry

The development and evaluation of new drug delivery systems (particularly with nanoscale materials) has been potentiating the advances in drug development. This special issue is meant to cover recent advances in development and application of nano delivery systems, peptide based delivery systems, self assembly of peptides structures and similar natural systems, Gene delivery, lipids, liposomes, miscelle, nanoparticular and carbon nanomaterials in drug delivery, mechanistic understanding of delivery systems, and other development of nanomaterials for drug delivery in medicinal chemistry.

Issue Editors:

Prof. Keykavous Parang
Associate Dean of Research, Graduate Studies, and Global Affairs
Professor of Medicinal Chemistry and Pharmacology
Harry and Diane Rinker Health Science Campus
9401 Jeronimo Rd. Irvine, CA 92618-1908. USA
Dindyal Mandal
Senior Research Associate
Harry and Diane Rinker Health Science Campus
9401 Jeronimo Rd. Irvine, CA 92618-1908. USA
Dr. B.S. Chhikara
Department of Chemistry,
University of Delhi, Aditi Mahavidyalaya,
Delhi 39. India

Submission

Article (Research articles and Review Articles) should be submitted online on the journal site http://www.pubs.thesciencein.org/journal/index.php/jmns as per author guidelines. Authors need to indicate submission to special issue in cover letter to editor.

Authors may also forward their final manuscript to editors via email ( bschhikara (at) gmail [dot] com )

Submission Deadline Submission ongoing, issue completion by March 2020

There is no publication charges for publishing in special issue.

Articles

Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy
Running Title: Rationale of designing of nanoparticular delivery systems and impact of chemistry used with doxorubicin for anti-cancer therapy
Bhupender S. Chhikara, Brijesh Rathi, Keykavous Parang

Synthesis, Characterization, Biocompatibility of Curcumin loaded Silica NP’s & their Therapeutic Applications: A Review
Parul Pant, Chetna Gupta, Sagar Kumar, Apoorva Grewal, Shivani Garg, Aishwarya Rai
(under process)

Current advances in drug delivery systems for treatment of Triple negative breast cancer (TNBC
Pooja Mittal, Sujata Singh, Archana Singh, Indrakant Kumar Singh
(under process)

Clinical and Pre-Clinical advances in Medicinal Chemistry – Special Issue Chemical Biology Letters

The medicinal Chemistry, the science concerned with development of new drug molecules, has produced many new drug entities recently which has reach in the clinical trial stages of evaluation. This special issue is meant to cover the research advances in development of new drug molecules and science behind it (including molecular modeling and pharmaceutical science) along with the research advances with new molecules that has shown promising potential to move to clinical applications.

Medicinal Chemistry fraternity is invited to submit their manuscript (Research Articles, Review Articles, and Short Communications) for publication in this special issue.

Issue Editors:

Dr. Brijesh Rathi,
Department of Chemistry, Hansraj College,
University of Delhi, Delhi-110007. India
Visiting Assistant Professor, Department of Chemistry
Massachusetts Institute of Technology (M.I.T.)
77 Massachusetts Ave. Cambridge, MA 02139, USA EB,
Dr. Prakasha Kempaiah,
Department of Medicine, Loyola University Medical Center
Health Sciences Division 2160 South 1st Avenue
Maywood, Chicago, IL 60153, USA


Submission

Article (Research articles and Review Articles) should be submitted online on the journal site http://www.pubs.thesciencein.org/journal/index.php/cbl as per author guidelines. Authors need to indicate submission to special issue in cover letter to editor.

Submission Deadline October 16, 2019

There is no publication charges for publishing in special issue or in Chemical Biology Letters.



Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy

Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy

Published in: Journal of Materials NanoScience

urn:nbn:sciencein.jmns.2019v6.95

Running title: Rationale of designing of nanoparticular delivery systems and impact of chemistry used with doxorubicin for anti-cancer therapy

  • Bhupender S. Chhikara University of Delhi
  • Brijesh Rathi University of Delhi
  • Keykavous Parang Chapman University

Keywords: Adriamycin, Cancer Drug, CPP, Drug Delivery System, Lipophilic Dox, TAT peptide

Abstract

Doxorubicin (Dox), an antineoplastic drug, has been extensively used for the treatment of different cancers. Dox is hydrophilic and therefore distributes to normal organs at a faster rate. Due to its required high doses, it poses severe toxicity, such as cardiotoxicity and nephrotoxicity. Diverse approaches, including nanoparticulate delivery systems, have been designed and evaluated to improve its delivery to the target site and reduce toxicity to normal organs; however, this has met little success. Here in this review, we have discussed various systems (metal nanoparticles, carbon nanotubes, fullerenes, liposomes, dendrimers, cyclic peptides, and other covalent/non-covalent systems) that have been used for Dox. We have critically evaluated their designing and outcome (in vitro and in vivo) with potential applications in the clinical setting.

Cite as: Chhikara, B., Rathi, B., & Parang, K. (2019). Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy. Journal of Materials NanoScience, 6(2), 47-66.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/95

Chemical libraries targeting Liver Stage Malarial infection

urn:nbn:sciencein.cbl.2019v6.96

Chemical Scaffolds Targeting liver-stage malaria parasite lifecycle

Published in: Chemical Biology Letters

  • Neha Sharma
  • Poonam FNU
  • Prakasha Kempaiah
  • Brijesh Rathi University of Delhi

Keywords: Malaria, Liver stage, Primaquine, Atovaquone, Clinical trials

Abstract

Despite the noteworthy advances in the use of chemotherapy for malaria, it continues to constantly affect large number of individuals. New molecules capable of blocking life-cycle of the parasite, preferably through targeting novel pathways and various modes of action, are increasingly becoming area of interest. Phenotypic screening of large chemical libraries is certainly one of the important criteria for the discovery of new and effective drugs. In recent years, diverse research groups including pharmaceutical industries have performed this large-scale phenotypic screening to identify the potential drug molecules. Most of the antimalarial drugs target blood-stage malarial infection and remain either less potent or ineffective against other life stages i.e. liver-stage, and the gametocyte stages of the parasite. Although, liver stage is considered as a crucial drug target, limited clinical options have significantly hampered the discovery of effective treatments. This short review presents the collection of selective molecules targeting specifically liver stage malaria parasites.

Cite as: Sharma, N., FNU, P., Kempaiah, P., & Rathi, B. (2019). Chemical libraries targeting Liver Stage Malarial infection. Chemical Biology Letters, 6(1), 14-22.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/96

NanoEnergy Journal Mat NanoScience – special issue

Nanoenergy is fast growing field with promises to bring new energy systems to meet the demand and define new technologies of future. The special issue of Nanoenergy cover the recent advances in the field and solicit articles from researchers related to following subfields:

Photovoltaic nanomaterials, Perovskite cells, Nanophotonics, Nanosolar cells, New nanomaterials for solar energy harvesting, Nanothermal energy systems, Nanosystems for harvesting mechanical and other forms of energy, Nanogenerator, higher efficiency nanomaterials for existing energy systems (production, transportation and storage), Nanostorage systems for energy, Nanobattery (design and development), Environmental issues concerned with nano energy systems, MEMS, Semiconductor design for energy systems, Carbon nanomaterials based energy generation and storage systems, new nanoenergy nanomaterials properties evaluation and all other research advances related to nanoenergy subtopics/

Editors of NanoEnergy special issue

Dr. Trilok Singh
School of Energy Science & Engineering
Sir J.C. Bose Laboratory Complex
Indian Institute of Technology Kharagpur Kharagpur – 721302, West Bengal, India
Dr. Bidhan Pramanick
Electrical Engineering Department
Indian Institute of Technology Goa, India
Dr. B.S. Chhikara
University of Delhi,
Delhi, India.

Manuscript Submission

Authors need to submit their manuscript in the NanoEnergy section of the journal. The manuscript should be formatted as per journal format provided in author guidelines section.

Article types: Research Article, Review Article, Short Communications, Experts Opinion article (contact editors before submission of Experts opinions articles).

Last date: The submissions are open now, author can submit their manuscript now, the last date for submissions to be considered in this issue is October 31.

Just to mention that There is no APC or authors fees for publication in the special issue.

Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines

urn:nbn:sciencein.cbl.2019v6.97

Published in: Chemical Biology Letters

  • P.J. Bindu Kuvempu University
  • T. R. Ravikumar Naik Indian Institute of Science
  • K.M. Mahadevan Kuvempu University
  • G. Krishnamurthy Sahyadri Science College

Keywords: Anti-oxidant, photodynamic therapy, DNA-Drug, tetrahydroquinolin

Abstract

2-Methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (3a−g) were synthesized by one pot multicomponent aza Diels-alder reaction between N-arylimines with two molecules of N-vinyl-2-pyrrolidinone in presence of Sm(III)nitrate as catalyst in acetonitrile solvent at room temperature stirring. The photocleavage studies with 2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (3a−g) revealed that almost all derivatives exhibited effective photocleavage of pUC−19 DNA at 365 nm, The The anticancer activities of newly synthesized compounds (3a−g) were more potent than doxorubicin on MCF−7 cells. The docking of PBR receptor (1EQ1) protein with newly synthesized THQ’s (3a-g) exhibited well established bonds with one or more amino acids in the receptor active pocket.

How to Cite Bindu, P., Naik, T. R. R., Mahadevan, K., & Krishnamurthy, G. (2019). Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines. Chemical Biology Letters, 6(1), 8-13.

Retrieve Full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/97