Special Issue on “Anticancer Drugs Activity and Underlying Mechanisms”

Iacopetta, Domenico

doi:10.3390/app11178169

Cited by 3 publications

(2 citation statements)

References 36 publications

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“…Despite the use of successful targeted and tailored therapies, many types of cancer, amongst them the triple negative breast cancers (TNBC), are still difficult to treat, mostly because of their heterogeneity and resistance onset [ 38 ]. A successful strategy in breast cancer therapy is based on the apoptosis induction in tumor cells acting on different pathways that are potential targets, with a minimal or null effect on the growth of the normal cells [ 39 , 40 ]. With this in mind, we studied the anticancer properties of a series of carbazole derivatives, ( 1 – 5 ), since our experience and a lot of studies from literature indicated their important antitumor activities, together with antibacterial, anti-inflammatory, and many other properties [ 8 , 20 , 41 , 42 ].…”

Section: Discussionmentioning

confidence: 99%

5,8-Dimethyl-9H-carbazole Derivatives Blocking hTopo I Activity and Actin Dynamics

et al. 2023

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Over the years, carbazoles have been largely studied for their numerous biological properties, including antibacterial, antimalarial, antioxidant, antidiabetic, neuroprotective, anticancer, and many more. Some of them have gained great interest for their anticancer activity in breast cancer due to their capability in inhibiting essential DNA-dependent enzymes, namely topoisomerases I and II. With this in mind, we studied the anticancer activity of a series of carbazole derivatives against two breast cancer cell lines, namely the triple negative MDA-MB-231 and MCF-7 cells. Compounds 3 and 4 were found to be the most active towards the MDA-MB-231 cell line without interfering with the normal counterpart. Using docking simulations, we assessed the ability of these carbazole derivatives to bind human topoisomerases I and II and actin. In vitro specific assays confirmed that the lead compounds selectively inhibited the human topoisomerase I and interfered with the normal organization of the actin system, triggering apoptosis as a final effect. Thus, compounds 3 and 4 are strong candidates for further drug development in multi-targeted therapy for the treatment of triple negative breast cancer, for which safe therapeutic regimens are not yet available.

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Section: Discussionmentioning

confidence: 99%

5,8-Dimethyl-9H-carbazole Derivatives Blocking hTopo I Activity and Actin Dynamics

et al. 2023

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“…However, the question posed by several readers, researchers, and patients is as follows: “Have any drugs that have been repurposed actually received approval for their new indications?” At first, one may find oneself engaged in confident mental processes, but with an impassive countenance, while seeking to recall enough examples to confirm the current reaction. Still, a memorable case, such as thalidomide, will spring to mind ( 4 ). The drug, infamously recognized in its devastating original form as a sedative and curative for morning sickness, returned to the medical world for the treatment of leprosy and, subsequently, multiple myeloma ( 5 ).…”

Section: Introductionmentioning

confidence: 99%

The dark side of drug repurposing. From clinical trial challenges to antimicrobial resistance: analysis based on three major fields

Natsheh,

Alsaleh,

Alkhawaldeh

et al. 2024

dti

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Drug repurposing is a strategic endeavor that entails the identification of novel therapeutic applications for pharmaceuticals that are already available in the market. Despite the advantageous nature of implement- ing this particular strategy owing to its cost-effectiveness and efficiency in reducing the time required for the drug discovery process, it is essential to bear in mind that there are various factors that must be meticulously considered and taken into account. Up to this point, there has been a noticeable absence of comprehensive analyses that shed light on the limitations of repurposing drugs. The primary aim of this review is to con- duct a thorough illustration of the various challenges that arise when contemplating drug repurposing from a clinical perspective in three major fields cardiovascular, cancer and diabetes and to further underscore the potential risks associated with the emergence of antimicrobial resistance when employing repurposed antibiotics for the treatment of noninfectious and infectious diseases. The process of developing repurposed medications necessitates the application of creativity and innovation in designing the development program, as the body of evidence may differ for each specific case. In order to effectively repurpose drugs, it is crucial to consider the clinical implications and potential drawbacks that may arise during this process. By com- prehensively analyzing these challenges, we can attain a deeper comprehension of the intricacies involved in drug repurposing, which will ultimately lead to the development of more efficacious and safe therapeutic approaches.

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Thiophene-Derived Schiff Base Complexes: Synthesis, Characterization, Antimicrobial Properties, and Molecular Docking

et al. 2023

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Novel thiophene-derived Schiff base ligand DE, where DE is (E)-N 1 ,N 1 -diethyl-N 2 -(thiophen-2-ylmethylene)ethane-1,2-diamine, and the corresponding M(II) complexes, [M(DE)X 2 ] (M = Cu or Zn, X = Cl; M = Cd, X = Br), were prepared and structurally characterized. X-ray diffraction studies revealed that the geometry around the center of the M(II) complexes, [Zn(DE)Cl 2 ] and [Cd(DE)Br 2 ], could be best described as a distorted tetrahedral. In vitro antimicrobial screening of DE and its corresponding M(II) complexes, [M(DE)X 2 ], was performed. The complexes were more potent and showed higher activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa, fungi Candida albicans, and protozoa Leishmania major compared to the ligand. Among the studied complexes, [Cd(DE)Br 2 ] exhibited the most promising antimicrobial activity against all the tested microbes compared to its analogs. These results were further supported by molecular docking studies. We believe that these complexes may significantly contribute to the efficient designing of metal-derived agents to treat microbial infections.

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Special Issue on “Anticancer Drugs Activity and Underlying Mechanisms”

Abstract: Cancer is a reputed non-communicable disease, namely a non-transmittable illness affecting humankind, which represents a major public health issue and is one of the leading causes of death worldwide [...]

Cited by 3 publications

References 36 publications

5,8-Dimethyl-9H-carbazole Derivatives Blocking hTopo I Activity and Actin Dynamics

5,8-Dimethyl-9H-carbazole Derivatives Blocking hTopo I Activity and Actin Dynamics

The dark side of drug repurposing. From clinical trial challenges to antimicrobial resistance: analysis based on three major fields

Thiophene-Derived Schiff Base Complexes: Synthesis, Characterization, Antimicrobial Properties, and Molecular Docking

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