A Triazaspirane Derivative Inhibits Migration and Invasion in PC3 Prostate Cancer Cells

Vasconcelos-Ulloa, Javier de Jesús; Salas, Benjamín Valdéz; Vazquez-Jimenez, J. Gustavo; Rivero-Espejel, Ignacio; Díaz-Molina, Raúl; Galindo-Hernández, Octavio

doi:10.3390/molecules28114524

Cited by 2 publications

(2 citation statements)

References 53 publications

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“…In this study, we put forth the proposition to assess diverse phenomena linked to the advancement of tumors. These phenomena encompass cell migration and invasion, which exhibit notable associations with the FAK/Src signaling pathway . At the same time, the Wnt/β-catenin pathway is a widely recognized oncogenic pathway.…”

Section: Experimental Sectionmentioning

confidence: 99%

“…These phenomena encompass cell migration and invasion, which exhibit notable associations with the FAK/Src signaling pathway. 39 At the same time, the Wnt/β-catenin pathway is a widely recognized oncogenic pathway. The inhibition of its growth has been regarded as a notable obstacle, particularly in the management of individuals diagnosed with colon cancer.…”

Section: Experimental Sectionmentioning

confidence: 99%

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Design, Synthesis, and In Silico and In Vitro Cytotoxic Activities of Novel Isoniazid–Hydrazone Analogues Linked to Fluorinated Sulfonate Esters

Başaran,

Tür,

Akkoc

et al. 2024

ACS Omega

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Cancer is a life-threatening disease, and significant efforts are still being made to treat it. In this study, we synthesized and characterized novel hybrid molecules (10−18) containing hydrazone and sulfonate moieties and tested their cell growth inhibitory effect on human colon cancer cells (DLD-1), human prostate cancer cells (PC3), and human embryonic kidney cells (HEK-293T) using the 3-(4,5-dimethylthiazol-2-yl)-2,5diphenyl tetrazolium bromide (MTT) method for 72 h. In cell culture studies, all tested hybrid molecules except for 12 and 13 showed significant cytotoxic activities at a micromolar level with IC 50 values in the range of 10.28−214.0 μM for the PC3 cell line and 13.49−144.30 μM for the DLD-1 cell line. Compounds 4 (10.28 μM) and 5 (11.22 μM) demonstrated the highest cytotoxicity against the PC3 cell line. Against the DLD-1 cell line, compounds 1 (22.53 μM), 4 (13.49 μM), 5 (19.33 μM), 6 (17.82 μM), 8 (24.71 μM), 9 (17.56 μM), and 10 (17.90 μM) in the series showed anticancer activity at lower micromolar levels compared to cisplatin (26.70 μM). Moreover, the study was handled computationally, and molecular docking studies were performed for compounds 1, 4, and 5 for PC3-FAK and PC3-Scr and compounds 4, 6, and 9 for the DLD-1-TNKS target. In this study, compound 4 was found to be the most effective and promising molecule for both targets.

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Section: Experimental Sectionmentioning

confidence: 99%

Section: Experimental Sectionmentioning

confidence: 99%

Design, Synthesis, and In Silico and In Vitro Cytotoxic Activities of Novel Isoniazid–Hydrazone Analogues Linked to Fluorinated Sulfonate Esters

Başaran,

Tür,

Akkoc

et al. 2024

ACS Omega

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Halloysite Nanotube-Based Delivery of Pyrazolo[3,4-d]pyrimidine Derivatives for Prostate and Bladder Cancer Treatment

Massaro,

Ciani,

Grossi

et al. 2024

Pharmaceutics

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Background/Objectives: The development of therapies targeting unregulated Src signaling through selective kinase inhibition using small-molecule inhibitors presents a significant challenge for the scientific community. Among these inhibitors, pyrazolo[3,4-d]pyrimidine heterocycles have emerged as potent agents; however, their clinical application is hindered by low solubility in water. To overcome this limitation, some carrier systems, such as halloysite nanotubes (HNTs), can be used. Methods: Herein, we report the development of HNT-based nanomaterials as carriers for pyrazolo[3,4-d]pyrimidine molecules. To achieve this objective, the clay was modified by two different approaches: supramolecular loading into the HNT lumen and covalent grafting onto the HNT external surface. The resulting nanomaterials were extensively characterized, and their morphology was imaged by high-angle annular dark-field scanning transmission electron microscopy (HAADF-STEM). In addition, the kinetic release of the molecules supramolecularly loaded into the HNTs was also evaluated. QSAR studies were conducted to elucidate the physicochemical and pharmacokinetic properties of these inhibitors, and structure-based virtual screening (SBVS) was performed to analyze their binding poses in protein kinases implicated in cancer. Results: The characterization methods demonstrate successful encapsulation of the drugs and the release properties under physiological conditions. Furthermore, QSAR studies and SBVS provide valuable insights into the physicochemical, pharmacokinetic, and binding properties of these inhibitors, reinforcing their potential efficacy. Conclusions: The cytotoxicity of these halloysite-based nanomaterials, and of pure molecules for comparison, was tested on RT112, UMUC3, and PC3 cancer cell lines, demonstrating their potential as effective agents for prostate and bladder cancer treatment.

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A Triazaspirane Derivative Inhibits Migration and Invasion in PC3 Prostate Cancer Cells

Cited by 2 publications

References 53 publications

Design, Synthesis, and In Silico and In Vitro Cytotoxic Activities of Novel Isoniazid–Hydrazone Analogues Linked to Fluorinated Sulfonate Esters

Design, Synthesis, and In Silico and In Vitro Cytotoxic Activities of Novel Isoniazid–Hydrazone Analogues Linked to Fluorinated Sulfonate Esters

Halloysite Nanotube-Based Delivery of Pyrazolo[3,4-d]pyrimidine Derivatives for Prostate and Bladder Cancer Treatment

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