1. Preliminary evaluation of antiproliferative and apoptotic activities of novel indolin-2-one derivatives.
- Author
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Turhal G, Demirkan B, Baslilar IN, Yuncu NS, Baytas SN, and Demiroglu-Zergeroglu A
- Subjects
- Humans, Cell Line, Tumor, Signal Transduction drug effects, Apoptosis drug effects, Cell Proliferation drug effects, Indoles pharmacology, Indoles chemistry, Antineoplastic Agents pharmacology, Antineoplastic Agents chemistry, Antineoplastic Agents chemical synthesis
- Abstract
Indole-based agents are frequently used in targeted or supportive therapy of several cancers. In this study, we investigated the anticancer properties of originally synthesized novel indolin-2-one derivatives (6a-d) against Malignant Mesothelioma, Breast cancer, and Colon Cancer cells. Our results revealed that all derivatives were effectively delayed cell proliferation by inhibiting the ERK1/2, AKT, and STAT3 signaling pathways in a concentration-dependent manner. Additionally, these variants induced cell cycle arrest in the S phase, accompanied by elevated levels of p21 and p27 expressions. Derivatives also initiated mitochondrial apoptosis through the upregulation of Bax and downregulation of Bcl-2 proteins, leading to the activation of caspase 3 and PARP cleavage in exposed cells. Remarkably, three of the indolin-2-one derivatives displayed significant selectivity towards Breast and Colon Cancer cells, with compound 6d promising as the most potent and wide spectral one for all cancer cell lines., (© 2024 The Author(s). Drug Development Research published by Wiley Periodicals LLC.)
- Published
- 2024
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