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Published on: June 9, 2023
Organoselenocyanate-Conjugated NBDHEX Derivatives as Potent Anticancer Agents for the Treatment of Breast Cancer via
Nikita Pal1, Rahul Kesarwani1, Tapas K Mandal2
1Department of Chemistry, Indian Institute of Technology Guwahati, Guwahati 781039, Assam, India.
Abstract:
Estrogen receptor-positive (ER+) breast cancer is the predominant subtype of breast cancer, having significant therapeutic drawbacks, largely driven by undesired toxicity and drug resistance associated with conventional treatment regimens. Conjugating organoselenium moieties to various drugs or enzyme inhibitors can be a promising approach for the treatment of breast cancer with multimodal benefits in overcoming the limitations of conventional therapies. Herein, we report the synthesis and evaluation of a series of organoselenium-NBDHEX hybrids as potent anticancer agents. Based on the selective antiproliferative activities of these derivatives against ER+ breast cancer cells (MCF-7) over the nonmalignant cells (L132), the hybrid NHSe-2, having a 2-selenocyanatoacetyl linker, was chosen as the lead analogue for further studies. The compound NHSe-2 exhibited notable antiproliferative activity with S-phase arrest of cells and late-phase apoptosis in MCF-7 cells. Most importantly, NHSe-2 induced ROS-mediated degradation of HDAC4, NF-κB, and c-Myc, resulting in potent antiproliferation and eventually leading to apoptosis of MCF-7 cells. Moreover, it suppressed β-catenin expression, unlike NBDHEX; however, it retained GSTP1 inhibitory potency, indicating its add-on therapeutic potential. Therefore, NHSe-2 could be a potential anticancer agent and can be considered for further analysis for its multimodal activity in the realm of cancer research in the future.
Insights
A novel organoselenium hybrid, NHSe-2, shows potent anticancer activity against estrogen receptor-positive breast cancer by inducing cell cycle arrest and apoptosis. This compound targets key proteins, offering a promising new therapeutic strategy for breast cancer treatment.
Area of Science:
- Oncology
- Medicinal Chemistry
- Biochemistry
Background:
- Estrogen receptor-positive (ER+) breast cancer is the most common subtype, often facing challenges with drug resistance and toxicity from conventional treatments.
- Organoselenium compounds offer a promising avenue for developing novel breast cancer therapies with multimodal benefits.
- Developing new agents to overcome limitations of current breast cancer treatments is crucial.
Purpose of the Study:
- To synthesize and evaluate novel organoselenium-NBDHEX hybrids as potential anticancer agents.
- To identify and characterize lead compounds with selective antiproliferative activity against ER+ breast cancer cells.
- To investigate the mechanism of action of the lead compound in ER+ breast cancer cells.
Main Methods:
- Synthesis of a series of organoselenium-NBDHEX hybrids.
- In vitro evaluation of antiproliferative activity against ER+ breast cancer cells (MCF-7) and nonmalignant cells (L132).
- Cell cycle analysis, apoptosis assays, and Western blotting to determine the mechanism of action.
Main Results:
- The hybrid NHSe-2 demonstrated selective antiproliferative activity against MCF-7 cells.
- NHSe-2 induced S-phase arrest and late-phase apoptosis in MCF-7 cells.
- NHSe-2 mediated ROS-dependent degradation of HDAC4, NF-κB, and c-Myc, suppressed β-catenin, and retained GSTP1 inhibitory activity.
Conclusions:
- NHSe-2 is a potent anticancer agent with multimodal activity against ER+ breast cancer.
- The compound's mechanism involves ROS-mediated degradation of key proteins and suppression of β-catenin.
- NHSe-2 warrants further investigation for its therapeutic potential in breast cancer treatment.
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