Impairing powerhouse in colon cancer cells by hydrazide–hydrazone-based small molecule
| Title | Impairing powerhouse in colon cancer cells by hydrazide–hydrazone-based small molecule |
| Publication Type | Journal Article |
| Year of Publication | 2018 |
| Authors | Patil, S, Kuman, MM, Palvai, S, Sengupta, P, Basu, S |
| Journal | ACS omega |
| Volume | 3 |
| Issue | 2 |
| Pagination | 1470–1481 |
| Date Published | FEB |
| Type of Article | Article |
| ISSN | 2470-1343 |
| 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 c. 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. |
| DOI | 10.1021/acsomega.7b01512 |
| Type of Journal (Indian or Foreign) | Foreign |
Divison category:
Physical and Materials Chemistry
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