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

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

Volume: 15 Issue: 8

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

Affiliation:

• Birla Institute of Technology and Sciences Pilani, Pilani Campus, Vidya Vihar, Pilani-333031, Rajasthan,India

• Birla Institute of Technology and Sciences Pilani, Pilani Campus, Vidya Vihar, Pilani-333031, Rajasthan,India

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

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.

Cite this article as:

Singh Mahaveer *, Jadhav R. Hemant *, Kumar Amit , Design, Synthesis and In vitro Evaluation of Piperazine Incorporated Novel Anticancer Agents, Letters in Drug Design & Discovery 2018; 15 (8) . https://dx.doi.org/10.2174/1570180815666171211161501