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Molecules
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Research and Development of Antibacterial and Antitumor Drugs
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Research and Development of Antibacterial and Antitumor Drugs

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: 31 July 2024 | Viewed by 1881

Special Issue Editors

Prof. Dr. Rozângela Curi Pedrosa

E-Mail Website
Guest Editor
Departamento de Bioquímica, Centro de Ciências Biológicas (CCB), Universidade Federal de Santa Catarina (UFSC), Florianópolis, SC, Brazil
Interests: cancer biology; cancer therapy; cancer chemotherapy; cancer cell line; cancer cells; cancer animal models
Prof. Dr. Ki-Young Kim

E-Mail Website
Guest Editor
Graduate School of Biotechnology, Kyung Hee University, Seocheon, Giheung, Yongin, Gyeonggi-do 1732, Republic of Korea
Interests: antimicrobial agents; anticancer agents; cell growth control; signal transduction; transcription regulation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibacterial agents have saved many lives and helped the growth of modern medicine over the past century, but the emergence of drug resistance threatens the effectiveness of these life-saving treatments. This highlights the urgent need for new and improved antibacterial drugs with novel targets.

Cancer is one of the leading causes of death worldwide. There are more than 100 types of cancer; this suggests that there are lots of way to suppress cancer occurrence and growth. Even though advances in diagnostic methods have allowed a substantial increase in patient survival, the increased occurrence of many types of malignant neoplasms and the poor responses to anti-cancer drug treatment in many patients, high costs, and side-effects result in new developmental requirements with new control methods.

In this Special Issue, original papers and reviews related to antibacterial and antitumor drugs are presented.

We kindly welcome all colleagues active in this field to contribute and also encourage authors to send their abstracts for pre-evaluation.

Please note that selected full papers will still be subjected to a thorough and rigorous peer review.

Prof. Dr. Rozângela Curi Pedrosa
Prof. Dr. Ki-Young Kim
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • antibacterial agent
  • antitumor drugs
  • resistance
  • target discovery
  • immune microenvironment
  • immuno-oncology
  • immunotherapy
  • tumor-associated macrophages
  • metastasis
  • combination therapy
  • precision medicine
  • anti-toxin
  • biofilm

Published Papers (2 papers)

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Research

12 pages, 2977 KiB  
Article
Design, Synthesis, Antifungal Activity, and 3D-QSAR Study of Novel Quinoxaline-2-Oxyacetate Hydrazide
by Peng Teng, Yufei Li, Ruoyu Fang, Yuchuan Zhu, Peng Dai and Weihua Zhang
Molecules 2024, 29(11), 2501; https://doi.org/10.3390/molecules29112501 - 25 May 2024
Viewed by 386
Abstract
Plant pathogenic fungi pose a major threat to global food security, ecosystem services, and human livelihoods. Effective and broad-spectrum fungicides are needed to combat these pathogens. In this study, a novel antifungal 2-oxyacetate hydrazide quinoxaline scaffold as a simple analogue was designed and [...] Read more.
Plant pathogenic fungi pose a major threat to global food security, ecosystem services, and human livelihoods. Effective and broad-spectrum fungicides are needed to combat these pathogens. In this study, a novel antifungal 2-oxyacetate hydrazide quinoxaline scaffold as a simple analogue was designed and synthesized. Their antifungal activities were evaluated against Botrytis cinerea (B. cinerea), Altemaria solani (A. solani), Gibberella zeae (G. zeae), Rhizoctonia solani (R. solani), Colletotrichum orbiculare (C. orbiculare), and Alternaria alternata (A. alternata). These results demonstrated that most compounds exhibited remarkable inhibitory activities and possessed better efficacy than ridylbacterin, such as compound 15 (EC50 = 0.87 μg/mL against G. zeae, EC50 = 1.01 μg/mL against C. orbiculare) and compound 1 (EC50 = 1.54 μg/mL against A. alternata, EC50 = 0.20 μg/mL against R. solani). The 3D-QSAR analysis of quinoxaline-2-oxyacetate hydrazide derivatives has provided new insights into the design and optimization of novel antifungal drug molecules based on quinoxaline. Full article
(This article belongs to the Special Issue Research and Development of Antibacterial and Antitumor Drugs)
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17 pages, 3505 KiB  
Article
Synthesis and Anticancer Evaluation of 4-Chloro-2-((5-aryl-1,3,4-oxadiazol-2-yl)amino)phenol Analogues: An Insight into Experimental and Theoretical Studies
by Obaid Afzal, Amena Ali, Abuzer Ali, Abdulmalik Saleh Alfawaz Altamimi, Manal A. Alossaimi, Md Afroz Bakht, Salahuddin, Mubarak A. Alamri, Md. Faiyaz Ahsan and Mohamed Jawed Ahsan
Molecules 2023, 28(16), 6086; https://doi.org/10.3390/molecules28166086 - 16 Aug 2023
Cited by 1 | Viewed by 1139
Abstract
We report herein the synthesis, docking studies and biological evaluation of a series of new 4-chloro-2-((5-aryl-1,3,4-oxadiazol-2-yl)amino)phenol analogues (6a-h). The new compounds were designed based on the oxadiazole-linked aryl core of tubulin inhibitors of IMC-038525 and IMC-094332, prepared in five steps and [...] Read more.
We report herein the synthesis, docking studies and biological evaluation of a series of new 4-chloro-2-((5-aryl-1,3,4-oxadiazol-2-yl)amino)phenol analogues (6a-h). The new compounds were designed based on the oxadiazole-linked aryl core of tubulin inhibitors of IMC-038525 and IMC-094332, prepared in five steps and further characterized via spectral analyses. The anticancer activity of the compounds was assessed against several cancer cell lines belonging to nine different panels as per National Cancer Institute (NCI US) protocol. 4-Chloro-2-((5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazol-2-yl)amino)phenol (6h) demonstrated significant anticancer activity against SNB-19 (PGI = 65.12), NCI-H460 (PGI = 55.61), and SNB-75 (PGI = 54.68) at 10 µM. The compounds were subjected to molecular docking studies against the active site of the tubulin–combretastatin A4 complex (PDB ID: 5LYJ); they displayed efficient binding and ligand 4h (with docking score = −8.030 kcal/mol) lay within the hydrophobic cavity surrounded by important residues Leu252, Ala250, Leu248, Leu242, Cys241, Val238, Ile318, Ala317, and Ala316. Furthermore, the antibacterial activity of some of the compounds was found to be promising. 4-Chloro-2-((5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl)amino)phenol (6c) displayed the most promising antibacterial activity against both Gram-negative as well as Gram-positive bacteria with MICs of 8 µg/mL and a zone of inhibition ranging from 17.0 ± 0.40 to 17.0 ± 0.15 mm at 200 µg/mL; however, the standard drug ciprofloxacin exhibited antibacterial activity with MIC values of 4 µg/mL. Full article
(This article belongs to the Special Issue Research and Development of Antibacterial and Antitumor Drugs)
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