Impairing Powerhouse in Colon Cancer Cells by Hydrazide-Hydrazone-Based Small Molecule.

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ID: 104495
2018
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Abstract
Mitochondrion has emerged as one of the unconventional targets in next-generation cancer therapy. Hence, small molecules targeting mitochondria in cancer cells have immense potential in the next-generation anticancer therapeutics. In this report, we have synthesized a library of hydrazide-hydrazone-based small molecules and identified a novel compound that induces mitochondrial outer membrane permeabilization by inhibiting antiapoptotic B-cell CLL/lymphoma 2 (Bcl-2) family proteins followed by sequestration of proapoptotic cytochrome . The new small molecule triggered programmed cell death (early and late apoptosis) through cell cycle arrest in the G2/M phase and caspase-9/3 cleavage in HCT-116 colon cancer cells, confirmed by an array of fluorescence confocal microscopy, cell sorting, and immunoblotting analysis. Furthermore, cell viability studies have verified that the small molecule rendered toxicity to a panel of colon cancer cells (HCT-116, DLD-1, and SW-620), keeping healthy L929 fibroblast cells unharmed. The novel small molecule has the potential to form a new understudied class of mitochondria targeting anticancer agent.
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patil2018impairingacs Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Patil, Sohan;Kuman, Meenu Mahesh;Palvai, Sandeep;Sengupta, Poulomi;Basu, Sudipta;
Journal ACS omega
Year 2018
DOI
10.1021/acsomega.7b01512
URL
Keywords
thiazole anti-proliferative estrone pyridine thiophene pim-1 kinase inhibitors

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