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Synthesis and Evaluation of Novel Anticancer and Anti-Inflammatory Agents
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Synthesis and Evaluation of Novel Anticancer and Anti-Inflammatory Agents

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Pharmaceutical Science".

Deadline for manuscript submissions: 30 November 2025 | Viewed by 2989

Special Issue Editors

Dr. Po-Jen Chen

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Guest Editor
Department of Medical Research, E-Da Hospital, Kaohsiung 824410, Taiwan
Interests: pharmacology; drug discovery; cancer biology; inflammation immunology
Dr. Yu-Chia Chang

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Guest Editor
Research Center for Chinese Herbal Medicine, College of Human Ecology, Chang Gung University of Science and Technology, Taoyuan 333324, Taiwan
Interests: natural product chemistry; liquid chromatography; mass spectrometry; new drugs’ development
Dr. Shun-Hua Chen

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Guest Editor
School of Nursing, Fooyin University, Kaohsiung 831301, Taiwan
Interests: cancer physiology; immunopharmacology; translational medicine
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The ongoing global burden of cancer and inflammatory diseases underscores the urgent need for novel therapeutic strategies. This Special Issue on the “Synthesis and Evaluation of Novel Anticancer and Anti-inflammatory Agents” aims to gather cutting-edge research focused on the design, synthesis, and biological evaluation of new anticancer and anti-inflammatory agents. We invite contributions that explore innovative approaches to drug discovery, including the development of small molecules, peptides, and other bioactive compounds with potential therapeutic applications. This Special Issue is particularly interested in studies that not only focus on synthetic methodologies but also emphasize the mechanisms of action, pharmacokinetics, and structure–activity relationships of these novel agents. Submissions that incorporate interdisciplinary approaches, combining medicinal chemistry, molecular biology, and pharmacology, are highly encouraged. By bringing together a diverse range of expertise, this Special Issue seeks to contribute to the advancement of effective treatments for cancer and inflammatory diseases, ultimately improving patient outcomes. We welcome original research articles, comprehensive reviews, and insightful perspectives that will enrich the understanding of these critical areas in drug development.

Dr. Po-Jen Chen
Dr. Yu-Chia Chang
Dr. Shun-Hua Chen
Guest Editors

Manuscript Submission Information

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Keywords

  • anticancer agents
  • anti-inflammatory agents
  • pharmacology
  • molecular and cell biology
  • drug design
  • medicinal chemistry
  • pharmacodynamics
  • pharmacokinetics
  • structure–activity relationship (SAR)

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Published Papers (3 papers)

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Research

16 pages, 2175 KiB  
Article
A New Class of BRCA1 Mimetics for ERα-Positive Breast Cancer Therapy: Design, Synthesis, In Silico Screening, In Vitro Assay, and Gene Expression Analysis
by Pottabathula Shyam Sundar, Jubie Selvaraj, Veerachamy Alagarsamy, Viswas Raja Solomon and Jawahar Natarajan
Life 2025, 15(4), 581; https://doi.org/10.3390/life15040581 - 1 Apr 2025
Viewed by 308
Abstract
Breast Cancer Gene 1 (BRCA1) offers a potential approach for ERα repression by blocking cyclin D1’s interaction with ERα, which prevents cells from growing and dividing too rapidly or uncontrollably. When BRCA1 levels are low, BRCA1 mimetics fit into the BRCA1-binding pocket within [...] Read more.
Breast Cancer Gene 1 (BRCA1) offers a potential approach for ERα repression by blocking cyclin D1’s interaction with ERα, which prevents cells from growing and dividing too rapidly or uncontrollably. When BRCA1 levels are low, BRCA1 mimetics fit into the BRCA1-binding pocket within ERα, mimicking the ability of BRCA1 to inhibit ERα activity. This study aims to identify a novel class of lead molecules for BRCA1 mimetics for ER-positive breast cancer, distinct from conventional antiestrogen therapies in their mechanism of action. In this article, coumarin thiosemicarbazone hybrids were synthesized from 7-hydroxy 4-methyl coumarin/4-hydroxy coumarin and thiosemicarbazide with different aldehydes and evaluated for their ERα repression activity. The most active compounds in the series, 9b, 9l, and 9m, exhibited significant potency with an IC50 value of 14.49 µM, 35.08 µM and 42.12 µM, respectively, compared to raloxifene (reported) as the positive control with an IC50 value of 13.7 µM. The gene expression study confirmed the downregulation of the cyclin D1 gene for the compounds 9l (−0.217) and 9m (−0.214). Similarly, the downregulation of the BCL2 gene for the compounds 9b (−0.373), 9l (−0.320), and 9m (−0.376). Also, molecular docking studies and MMGBSA were performed to determine key interactions between compounds and ERα at the BRCA1 binding pocket (AA 338–387). In silico, ADMET properties were executed to illustrate the druggability and safety of the novel derivatives. In silico, in vitro, and gene expression studies revealed that among all the compounds, 9b, 9l, and 9m are promising candidates for the development of lead molecules targeting ERα inhibitors for breast cancer treatment. Moreover, the concept of ERα repression with small molecules as BRCA1 mimetics is novel. In general, it can be concluded that these compounds can serve as promising leads to the design of potential BRCA1 mimetics. Full article
(This article belongs to the Special Issue Synthesis and Evaluation of Novel Anticancer and Anti-Inflammatory Agents)
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16 pages, 5763 KiB  
Article
Anti-Inflammatory Potential and Synergic Activities of Eclipta prostrata (L.) L. Leaf-Derived Ointment Formulation in Combination with the Non-Steroidal Anti-Inflammatory Drug Diclofenac in Suppressing Atopic Dermatitis (AD)
by Muhammad M. Poyil, Mohammed H. Karrar Alsharif, Mahmoud H. El-Bidawy, Salman Bin Dayel, Mohammed Sarosh Khan, Zainab Mohammed M. Omar, Alaaeldin Ahmed Mohamed, Reda M. Fayyad, Tarig Gasim Mohamed Alarabi, Hesham A. Khairy, Nasraddin Othman Bahakim, Mohamed A. Samhan and Abd El-Lateef Saeed Abd El-Lateef
Life 2025, 15(1), 35; https://doi.org/10.3390/life15010035 - 30 Dec 2024
Cited by 1 | Viewed by 1117
Abstract
Atopic dermatitis (AD) or eczema is an important inflammatory chronic skin disease that brings many complications in its management and treatment. Although several chemical agents are used for treatment, the search for better anti-inflammatory and antibacterial agents of plant origin has been ongoing, [...] Read more.
Atopic dermatitis (AD) or eczema is an important inflammatory chronic skin disease that brings many complications in its management and treatment. Although several chemical agents are used for treatment, the search for better anti-inflammatory and antibacterial agents of plant origin has been ongoing, since natural compounds, it is commonly believed, are less dangerous than synthetic ones. Therefore, the present study explored a medicinal plant—Eclipta prostrata (L.) L.—for its anti-inflammatory activity alone and in combination with a non-steroidal anti-inflammatory drug (NSAID), diclofenac. The plant extract was used to make a cream formulation for treating atopic dermatitis and as an antibacterial agent against Staphylococcus aures, the major infectious agent associated with AD. The phytochemical analysis of the E. prostrata extract showed the presence of various phytochemicals, including flavonoids, Tannin, saponin, terpenoids, glycosides, phenol, alkaloids, quinone, and protein. The GC-MS profiling of methanolic E. prostrata extract was performed predicted the presence of twenty important phytochemicals, including 2-[5-(2-Hydroxypropyl) oxolan-2-yl]propanoic acid, dl-Menthol, dodecane, undecane, 4,7-dimethyl-, dodecane, 2,6,10-trimethyl-, decane, 2,3,5,8-tetramethyl-, cholest-5-en-3-ol, (3.alpha.)-, TMS derivative, cyclopropane carboxylic acid, 1-hydroxy-, (2,6-di-t-butyl-4-methylphenyl) ester, alpha.-farnesene, propanoic acid, 2-methyl-, 2-ethyl-1-propyl-1,3-propanediyl ester, diethyl phthalate, corticosterone, 2-methylpropionate, hentriacontan-13-ol, O-TMS, phthalic acid, 2,4-dimethylpent-3-yl dodecyl ester, hexasiloxane, 1,1,3,3,5,5,7,7,9,9,11,11-dodecamethyl-, acetic acid, 4-t-butyl-4-hydroxy-1,5-dimethyl-hex-2-ynyl ester, octadecane, 2-methyl- octacosane, 1-iodo-, nonacosane, and eicosyl isopropyl ether. Using an egg albumin denaturation inhibition assay, the anti-inflammatory activities of E. prostrata alone and in combination with diclofenac were investigated, and they showed 93% and 99% denaturation inhibition at 5 mg concentration of E. prostrata in alone and combination with diclofenac, respectively. Heat-induced haemolysis showed 2.5% and 2.4% of haemolysis at 5 mg of E. prostrata alone and in combination with diclofenac, respectively. An MTT assay performed using L929 cells proved that the extract has no cytotoxic effect. The plant extract displayed potential antibacterial activity against Staphylococcus aureus; the growth was inhibited at 1 mg/mL of E. prostrata extract. Thus, based on this evidence, the authors suggest that E. prostrata extract should be studied further for its anti-inflammatory and antibacterial activities and topical application in the treatment of atopic dermatitis. Full article
(This article belongs to the Special Issue Synthesis and Evaluation of Novel Anticancer and Anti-Inflammatory Agents)
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19 pages, 8386 KiB  
Article
Eradication of Biofilms on Catheters: Potentials of Tamarix ericoides Rottl. Bark Coating in Preventing Catheter-Associated Urinary Tract Infections (CAUTIs)
by Mohammed H. Karrar Alsharif, Muhammad Musthafa Poyil, Salman Bin Dayel, Mohammed Saad Alqahtani, Ahmed Abdullah Albadrani, Zainab Mohammed M. Omar, Abdullah MR. Arafah, Tarig Gasim Mohamed Alarabi, Reda M. Fayyad and Abd El-Lateef Saeed Abd El-Lateef
Life 2024, 14(12), 1593; https://doi.org/10.3390/life14121593 - 3 Dec 2024
Viewed by 1099
Abstract
Catheter-associated urinary tract infections (CAUTIs) cause serious complications among hospitalized patients due to biofilm-forming microorganisms which make treatment ineffective by forming antibiotic-resistant strains. As most CAUTI-causing bacterial pathogens have already developed multidrug resistance, there is an urgent need for alternative antibacterial agents to [...] Read more.
Catheter-associated urinary tract infections (CAUTIs) cause serious complications among hospitalized patients due to biofilm-forming microorganisms which make treatment ineffective by forming antibiotic-resistant strains. As most CAUTI-causing bacterial pathogens have already developed multidrug resistance, there is an urgent need for alternative antibacterial agents to prevent biofilms on catheter surfaces. As a trial to find out such a potential agent of natural origin, the bark of Tamarix ericoides Rottl., a little-known plant from the Tamaricaceae family, was examined for its antibacterial and antibiofilm activities against one of the major, virulent, CAUTI-causing bacterial pathogens: Enterococcus faecalis. The methanolic T. ericoides bark extract was analyzed for its antibacterial activity using the well diffusion method and microdilution method. Killing kinetics were calculated using time–kill assay, and the ability of biofilm formation and its eradication upon treatment with the T. ericoides bark extract was studied by crystal violet assay. GC-MS analysis was performed to understand the phytochemical presence in the extract. A in vitro bladder model study was performed using extract-coated catheters against E. faecalis, and the effect was visualized using CLSM. The changes in the cell morphology of the bacterium after treatment with the T. ericoides bark extract were observed using SEM. The biocompatibility of the extract towards L929 cells was studied by MTT assay. The anti-E. faecalis activity of the extract-coated catheter tube was quantified by viable cell count method, which exposed 20% of growth after five days of contact with E. faecalis. The anti-adhesive property of the T. ericoides bark extract was studied using CLSM. The extract showed potential antibacterial activity, and the lowest inhibitory concentration needed to inhibit the growth of E. faecalis was found to be 2 mg/mL. The GC-MS analysis of the methanolic fractions of the T. ericoides bark extract revealed the presence of major phytochemicals, such as diethyl phthalate, pentadecanoic acid, methyl 6,11-octadecadienoate, cyclopropaneoctanoic acid, 2-[(2-pentylcyclopropyl) methyl]-, methyl ester, erythro-7,8-bromochlorodisparlure, etc., that could be responsible for the antibacterial activity against E. faecalis. The killing kinetics of the extract against E. faecalis was calculated and the extract showed promising antibiofilm activity on polystyrene surfaces. The T. ericoides bark extract effectively reduced the E. faecalis mature biofilms by 75%, 82%, and 83% after treatment with 1X MIC (2 mg/mL), 2X MIC (4 mg/mL), and 3X MIC (6 mg/mL) concentrations, respectively, which was further confirmed by SEM analysis. The anti-adhesive property of the T. ericoides bark extract studied using CLSM revealed a reduction in the biofilm thickness, and the FDA and PI combination revealed the death of 80% of the cells on the extract-coated catheter tube. In addition, SEM analysis showed extensive damage to the E. faecalis cells after the T. ericoides bark extract treatment, and it was not cytotoxic. Hence, after further studies, T. ericoides bark extract with potential antibacterial, antibiofilm, and anti-adhesive activities can be developed as an alternative agent for treating CAUTIs. Full article
(This article belongs to the Special Issue Synthesis and Evaluation of Novel Anticancer and Anti-Inflammatory Agents)
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