Article ; Online: Piperazine clubbed with 2-azetidinone derivatives suppresses proliferation, migration and induces apoptosis in human cervical cancer HeLa cells through oxidative stress mediated intrinsic mitochondrial pathway.
Apoptosis : an international journal on programmed cell death
2018 Volume 23, Issue 2, Page(s) 113–131
Abstract: Piperazine scaffolds or 2-azetidinone pharmacophores have been reported to show anti-cancer activities and apoptosis induction in different types of cancer cells. However, the mechanistic studies involve in induction of apoptosis addressing these two ... ...
| Abstract | Piperazine scaffolds or 2-azetidinone pharmacophores have been reported to show anti-cancer activities and apoptosis induction in different types of cancer cells. However, the mechanistic studies involve in induction of apoptosis addressing these two moieties for human cervical cancer cells remain uncertain. The present study emphasizes on the anti-proliferating properties and mechanism involved in induction of apoptosis for these structurally related azoles derivatives in HeLa cancer cells. 1-Phenylpiperazine clubbed with 2-azetidione derivatives (5a-5h) were synthesized, characterized using various spectroscopic techniques and evaluated for their in-vitro anti-proliferative activities and induction of apoptosis. Further, we also evaluated oxidative stress generated by these synthetic derivatives (5a-5h). Cell viability studies revealed that among all, the compound N-(3-chloro-2-(3-nitrophenyl)-4-oxoazetidin-1-yl)-2-(4-phenylpiperazin-1-yl) acetamide 5e remarkably inhibited the growth of HeLa cells in a concentration dependent manner having IC |
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| MeSH term(s) | Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Azetidines/chemical synthesis ; Azetidines/chemistry ; Azetidines/pharmacology ; Caspase 3/genetics ; Caspase 3/metabolism ; Cell Cycle Checkpoints/drug effects ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; DNA Fragmentation/drug effects ; Female ; HeLa Cells ; Humans ; Mitochondria/drug effects ; Mitochondria/genetics ; Mitochondria/metabolism ; Oxidative Stress/drug effects ; Piperazine/analogs & derivatives ; Piperazine/chemical synthesis ; Piperazine/pharmacology ; Reactive Oxygen Species/metabolism ; Uterine Cervical Neoplasms/genetics ; Uterine Cervical Neoplasms/metabolism ; Uterine Cervical Neoplasms/physiopathology | |||||
| Chemical Substances | 2-azetidinone ; Antineoplastic Agents ; Azetidines ; Reactive Oxygen Species ; Piperazine (1RTM4PAL0V) ; CASP3 protein, human (EC 3.4.22.-) ; Caspase 3 (EC 3.4.22.-) | |||||
| Language | English | |||||
| Publishing date | 2018-01-18 | |||||
| Publishing country | Netherlands | |||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | |||||
| ZDB-ID | 1452360-7 | |||||
| ISSN | 1573-675X ; 1360-8185 | |||||
| ISSN (online) | 1573-675X | |||||
| ISSN | 1360-8185 | |||||
| DOI | 10.1007/s10495-018-1439-x | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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