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.
