Design, Synthesis and In vitro Evaluation of Piperazine Incorporated Novel Anticancer Agents

Author(s): Mahaveer Singh*, Hemant R. Jadhav*, Amit Kumar

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 8 , 2018

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Graphical Abstract:


Background: Novel 4-(3-(4-ethylpiperazin-1-yl)propoxy)-N-phenylbenzamide derivatives (C-1 to C-10) and (4-(3-(4-ethylpiperazin-1-yl)propoxy)phenyl)(4-(2-methoxyphenyl)piperazin-1- yl)ethanone derivatives (C-11 to C-16) were designed and synthesized by pharmacophore approach.

Methods: All compounds were evaluated for their in-vitro cytotoxicity against a panel of three cancer cell lines (A-549 human lung carcinoma, HCT-116 colon cancer and pancreatic cancer MIAPaCa-2).

Results: The results indicated that in A-549 human lung carcinoma cell line, compounds C-4 and C-5 showed IC50 values of 33.20µM and 21.22µM, respectively, which is comparable to standard (gefitinib, IC50 value: 16.56 µM). These compounds, in HCT-116 colon cancer line, showed IC50 values of 11.33µM and 45.89µM which was again comparable to gefitinib that showed IC50 value of 10.51µM. Also, in MIAPaCa-2 cell line, compound C-14 showed IC50 value of <1µM. To give mechanistic basis, in silico docking studies were done and it shows good in silico – in vitro correlation.

Conclusion: These results provide an encouraging lead that could be used for the development of new potent anticancer agents.

Keywords: Carcinoma, cytotoxocity, epidermal growth factor receptor inhibitors, gefitinib, ethyl piperazine, cancer line.

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Article Details

Year: 2018
Published on: 21 June, 2018
Page: [866 - 874]
Pages: 9
DOI: 10.2174/1570180815666171211161501
Price: $65

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