Title |
Synthesis, DNA-binding abilities and anticancer activities of triazole-pyrrolo[2,1-c][1,4]benzodiazepines hybrid scaffolds
|
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Published in |
Bioorganic & Medicinal Chemistry Letters, October 2013
|
DOI | 10.1016/j.bmcl.2013.10.004 |
Pubmed ID | |
Authors |
Chung-Yu Chen, Pei-Hua Lee, Yong-Yong Lin, Wen-Ting Yu, Wan-Ping Hu, Chia-Chen Hsu, Ying-Ting Lin, Long-Sen Chang, Cheng-Tien Hsiao, Jeh-Jeng Wang, Mei-Ing Chung |
Abstract |
We synthesized a new series of PBD-hybrid derivatives having tethered triazoles and investigated for their cytotoxicity. The studies indicated that cis-olefin compounds induce higher cytotoxicity with increase in the G1 cell cycle phase compared with the trans-compounds. Quantitative RT-PCR assay indicated that compounds (16a-d) induced G1 phase arrest through down-regulation of cyclin D1 and up-regulation of p21, p27, and p53 mRNA expressions. Compounds 16a-d induced A375 early apoptosis as detected by flow cytometry after double-staining with annexin V and propidium iodide. Moreover, the Western blot analysis showed that A375 treated by compounds (16a-d) resulted in decreased levels of Bcl-2 and Bcl-xL, increased levels of Bax and Bad, and caspase/PARP degradation to identify apoptotic cells. |
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Demographic breakdown
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