Drug Candidates for the Treatment of Breast Cancer

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 6950

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School of Medicine, I-Shou University, Kaohsiung 82445, Taiwan
Interests: molecular biology of cancer; tumor pathology; molecular diagnosis; new drug research and development; health medical data analysis
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Special Issue Information

Dear Colleagues,

Breast cancer has become the most commonly diagnosed cancer globally, and the incidence and number of survivors with this disease continue to increase, with most developed countries reporting 85–90% five-year survival rates. Both the relapse and metastasis of breast cancer remain great challenges, despite advances in chemoprevention, chemotherapy, endocrine therapy, and gene-targeted therapy over the past decades. Innovative therapeutic strategies are still urgently needed. Cancer vaccines and new drugs are attractive options, as they aim to induce a durable response or therapeutic relevance to eradicate breast cancer.

We welcome articles pertaining to the development of novel pharmacologically active compounds, and the continued use of natural products, as well as synthetic and existing drugs as new drug developments for breast cancer treatment.  We also welcome review and original articles that highlight the challenges and opportunities in the development of breast cancer treatment drugs. The topics of interest include, but are not limited to, the following: new positioning of breast cancer treatment drugs; selective optimization and reduction of side effects; the origin and application of synthetic drugs or drug metabolites as new drugs, drug delivery systems, or for nanomaterial applications. The collection of manuscripts will be published as a Special Issue in the journal.

Prof. Dr. Yi-Chiang Hsu
Guest Editor

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Keywords

  • breast cancer
  • tumor antigens
  • vaccine
  • metastasis
  • nanotechnology

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Published Papers (2 papers)

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Research

30 pages, 9061 KiB  
Article
Achillea fragrantissima (Forssk.) Sch.Bip Flower Dichloromethane Extract Exerts Anti-Proliferative and Pro-Apoptotic Properties in Human Triple-Negative Breast Cancer (MDA-MB-231) Cells: In Vitro and In Silico Studies
by Nora Alshuail, Zeyad Alehaideb, Sahar Alghamdi, Rasha Suliman, Hamad Al-Eidi, Rizwan Ali, Tlili Barhoumi, Mansour Almutairi, Mona Alwhibi, Bandar Alghanem, Abir Alamro, Amani Alghamdi and Sabine Matou-Nasri
Pharmaceuticals 2022, 15(9), 1060; https://doi.org/10.3390/ph15091060 - 26 Aug 2022
Cited by 14 | Viewed by 3059
Abstract
The aggressive triple-negative breast cancer (TNBC) is a challenging disease due to the absence of tailored therapy. The search for new therapies involves intensive research focusing on natural sources. Achillea fragrantissima (A. fragrantissima) is a traditional medicine from the Middle East [...] Read more.
The aggressive triple-negative breast cancer (TNBC) is a challenging disease due to the absence of tailored therapy. The search for new therapies involves intensive research focusing on natural sources. Achillea fragrantissima (A. fragrantissima) is a traditional medicine from the Middle East region. Various solvent extracts from different A. fragrantissima plant parts, including flowers, leaves, and roots, were tested on TNBC MDA-MB-231 cells. Using liquid chromatography, the fingerprinting revealed rich and diverse compositions for A. fragrantissima plant parts using polar to non-polar solvent extracts indicating possible differences in bioactivities. Using the CellTiter-Glo™ viability assay, the half-maximal inhibitory concentration (IC50) values were determined for each extract and ranged from 32.4 to 161.7 µg/mL. The A. fragrantissima flower dichloromethane extract had the lowest mean IC50 value and was chosen for further investigation. Upon treatment with increasing A. fragrantissima flower dichloromethane extract concentrations, the MDA-MB-231 cells displayed, in a dose-dependent manner, enhanced morphological and biochemical hallmarks of apoptosis, including cell shrinkage, phosphatidylserine exposure, caspase activity, and mitochondrial outer membrane permeabilization, assessed using phase-contrast microscopy, fluorescence-activated single-cell sorting analysis, Image-iT™ live caspase, and mitochondrial transition pore opening activity, respectively. Anticancer target prediction and molecular docking studies revealed the inhibitory activity of a few A. fragrantissima flower dichloromethane extract-derived metabolites against carbonic anhydrase IX, an enzyme reported for its anti-apoptotic properties. In conclusion, these findings suggest promising therapeutic values of the A. fragrantissima flower dichloromethane extract against TNBC development. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Breast Cancer)
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23 pages, 3399 KiB  
Article
Dihydropyrazole-Carbohydrazide Derivatives with Dual Activity as Antioxidant and Anti-Proliferative Drugs on Breast Cancer Targeting the HDAC6
by Irving Balbuena-Rebolledo, Astrid M. Rivera-Antonio, Yudibeth Sixto-López, José Correa-Basurto, Martha C. Rosales-Hernández, Jessica Elena Mendieta-Wejebe, Francisco J. Martínez-Martínez, Ivonne María Olivares-Corichi, José Rubén García-Sánchez, Juan Alberto Guevara-Salazar, Martiniano Bello and Itzia I. Padilla-Martínez
Pharmaceuticals 2022, 15(6), 690; https://doi.org/10.3390/ph15060690 - 31 May 2022
Cited by 5 | Viewed by 3254
Abstract
Breast cancer (BC) is the most frequently diagnosed cancer and is the second-most common cause of death in women worldwide. Because of this, the search for new drugs and targeted therapy to treat BC is an urgent and global need. Histone deacetylase 6 [...] Read more.
Breast cancer (BC) is the most frequently diagnosed cancer and is the second-most common cause of death in women worldwide. Because of this, the search for new drugs and targeted therapy to treat BC is an urgent and global need. Histone deacetylase 6 (HDAC6) is a promising anti-BC drug target associated with its development and progression. In the present work, the design and synthesis of a new family of dihydropyrazole-carbohydrazide derivatives (DPCH) derivatives focused on HDAC6 inhibitory activity is presented. Computational chemistry approaches were employed to rationalize the design and evaluate their physicochemical and toxic-biological properties. The new family of nine DPCH was synthesized and characterized. Compounds exhibited optimal physicochemical and toxicobiological properties for potential application as drugs to be used in humans. The in silico studies showed that compounds with –Br, –Cl, and –OH substituents had good affinity with the catalytic domain 2 of HDAC6 like the reference compounds. Nine DPCH derivatives were assayed on MCF-7 and MDA-MB-231 BC cell lines, showing antiproliferative activity with IC50 at μM range. Compound 2b showed, in vitro, an IC50 value of 12 ± 3 µM on human HDAC6. The antioxidant activity of DPCH derivatives showed that all the compounds exhibit antioxidant activity similar to that of ascorbic acid. In conclusion, the DPCH derivatives are promising drugs with therapeutic potential for the epigenetic treatment of BC, with low cytotoxicity towards healthy cells and important antioxidant activity. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Breast Cancer)
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