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Research Progress in Bioorganic Medicinal Chemistry
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Research Progress in Bioorganic Medicinal Chemistry

A special issue of Sci (ISSN 2413-4155). This special issue belongs to the section "Biology Research and Life Sciences".

Deadline for manuscript submissions: closed (15 November 2022) | Viewed by 4768

Special Issue Editors

Prof. Dr. Amandeep Arora

E-Mail Website
Guest Editor
Department of Natural and Applied Science, University of Dubuque, 104E University Science Center, 2000 University Ave, Dubuque, IA 001891, USA
Interests: catalysis; photoredox; green chemistry; teaching based education
Dr. Amandeep Singh

E-Mail Website
Guest Editor
Department of Pharmacology, College of Medicine, Penn State University, Hershey, PA 17033, USA
Interests: medicinal chemistry; organic synthesis; pharmacology; drug discovery; molecular docking; anti-cancer activities
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues

We are pleased to invite you to contribute to the Sci Special Issue ‘Research Progress in Bioorganic Medicinal Chemistry’. We welcome the submission of both original research and critical review articles for possible publication in the Issue.

Topics of interest for this Issue include:

  • Discovery or advancement for first-in-class new medicinal or biological agents;
  • Advancing new chemical reactions or new synthetic routes that impact medicine;
  • Advancing new biological mechanisms in medicine;
  • Structure–activity relationship or pharmacological issues analysis (including computational) and discussions relevant to drug design and development;
  • Development of new materials for therapeutic targets.

Prof. Dr. Amandeep Arora
Dr. Amandeep Singh
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Sci is an international peer-reviewed open access quarterly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1200 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • drug delivery
  • synthesis
  • medicinal chemistry
  • pharmacology
  • toxicology
  • natural products

Published Papers (2 papers)

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Research

14 pages, 2369 KiB  
Article
A Histone Deacetylase Inhibitor Manifests Synergistic Interaction with Artesunate by Suppressing DNA Repair Activity
by Asif Raza, Raghuram Kandimalla, Sanjeeb Kalita and Siddhartha Sankar Ghosh
Sci 2022, 4(4), 41; https://doi.org/10.3390/sci4040041 - 26 Oct 2022
Viewed by 1665
Abstract
Artesunate (ART), a plant based semi-synthetic antimalarial drug, is emerging as a new class of effective cancer chemotherapeutics. However, the dosage of ART required to have an anti-cancer effect on cancer cells is greater than that needed to exterminate malarial parasites. The goal [...] Read more.
Artesunate (ART), a plant based semi-synthetic antimalarial drug, is emerging as a new class of effective cancer chemotherapeutics. However, the dosage of ART required to have an anti-cancer effect on cancer cells is greater than that needed to exterminate malarial parasites. The goal of this study was to develop an effective combination therapy to reduce the dose-dependent side effects of ART both in vitro and in vivo. In our study, 4-phenylbutyrate (4-PB), a histone deacetylase inhibitor (HDAC), exhibited significant synergistic induction of apoptosis in MCF-7 cells in combination with ART. The IC50 of ART decreased significantly from 55.56 ± 5.21 µM to 24.71 ± 3.44 µM in MCF-7 cells. ART treatment increased cellular oxidative stress, and the resulting generation of intracellular reactive oxygen species (ROS) caused extensive DNA damage in the cell. The extent of ROS production and cell cycle arrest were further enhanced by 4-PB treatment. In further investigation, we found that 4-PB attenuated mRNA expression of crucial DNA damage response (DDR) elements of the nonhomologous end-joining (NHEJ) pathway, consequently enhancing the DNA damaging effect of ART. Furthermore, the combination therapy resulted in improvement in the life expectancy of the treated mice and a prominent reduction in tumour volume without interfering with the normal biochemical, haematological and histological parameters of the mice. Overall, our study revealed a novel combination therapy in which 4-PB potentiated the cytotoxicity of ART synergistically and provided a promising combination drug for effective cancer therapy. Full article
(This article belongs to the Special Issue Research Progress in Bioorganic Medicinal Chemistry)
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15 pages, 2875 KiB  
Communication
Trifluoromethylated Quinolone-Hydantoin Hybrids: Synthesis and Antibacterial Evaluation
by Akhil Mahajan, Harbinder Singh, Amandeep Singh, Devendra K. Agrawal, Amandeep Arora and Tejpal Singh Chundawat
Sci 2022, 4(3), 30; https://doi.org/10.3390/sci4030030 - 18 Jul 2022
Cited by 7 | Viewed by 2540
Abstract
A series of new trifluoromethyl-substituted quinolones and hydantoin hybrids has been synthesized and evaluated against Gram-positive bacterium (Staphylococcus aureus MTCC 96) and Gram-negative bacteria (Pseudomonas aeruginosa MTCC 441, Klebsiella pneumonia MTCC 109, and Escherichia coli MTCC 442). Compound  19c, [...] Read more.
A series of new trifluoromethyl-substituted quinolones and hydantoin hybrids has been synthesized and evaluated against Gram-positive bacterium (Staphylococcus aureus MTCC 96) and Gram-negative bacteria (Pseudomonas aeruginosa MTCC 441, Klebsiella pneumonia MTCC 109, and Escherichia coli MTCC 442). Compound  19c, having the 6-propene group on the quinolone ring, showed similar activity to a standard drug (chloramphenicol) by exhibiting MIC values of 50 µg/mL against S. aureus and P. aeruginosa. Physicochemical properties of compound 19c were also determined, which were in line with Lipinski’s rule of five, suggesting the suitability of compound 19c in biological systems. Various types of binding interactions of 19c within the active site of DNA gyrase of S. aureus were also streamlined by molecular docking studies, suggesting its capability to block the catalytic process of the DNA gyrase, which could be the possible reason for its antibacterial potential. Full article
(This article belongs to the Special Issue Research Progress in Bioorganic Medicinal Chemistry)
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