Citation: Taha Muhammad, Ali Shah Syed Adnan, Afifi Muhammad, Zulkeflee Manar, Sultan Sadia, Wadood Abdul, Rahim Fazal, Ismail Nor Hadiani. Morpholine hydrazone scaffold: Synthesis, anticancer activity and docking studies[J]. Chinese Chemical Letters, ;2017, 28(3): 607-611. doi: 10.1016/j.cclet.2016.10.020 shu

Morpholine hydrazone scaffold: Synthesis, anticancer activity and docking studies

a.
Atta-ur-Rahman Institute for Natural Product Discovery (AuRIns), Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D. E., Malaysia
b.
Faculty of Applied Science, UiTM Shah Alam, 40450 Shah Alam, Selangor D. E., Malaysia
c.
Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D. E., Malaysia
d.
Department of Biochemistry, Abdul Wali Khan University, Mardan 23200, Pakistan
e.
Department of Chemistry, Hazara University, Mansehra 21300, Pakistan

Corresponding author: Taha Muhammad, taha_hej@yahoo.com Ali Shah Syed Adnan, syedadnan@salam.uitm.edu.my
Received Date: 17 June 2016
Revised Date: 22 August 2016
Accepted Date: 12 September 2016
Available Online: 20 March 2016

Figures(2)

In this paper, synthesis and anticancer activities of morpholine hydrazones scaffold (1-17) thoroughly studied. Small series of morpholine hydrazones synthesized by treating 5-morpholinothiophene-2-carbaldehyde with different aryl hydrazides to form morpholine hydrazones scaffold (1-17). The in vitro anticancer potential of all these compounds was checked against human cancer cell lines like HepG2 (human hepatocellular liver carcinoma) and MCF-7 (human breast adenocarcinoma). Analogs 13 had similar substantial cytotoxic effects towards HepG2 with IC₅₀ value 6.31±1.03 μmol/L when compared with the standard Doxorubicin (IC₅₀ value 6.00±0.80 μmol/L); while compounds 5, 8 and 9 showed potent cytotoxicity against MCF-7 with IC₅₀ value 7.08±0.42 μmol/L, 1.26±0.34 μmol/L and 11.22±0.22 μmol/L respectively when compared with the standard Tamoxifen (IC₅₀=11.00±0.40 μmol/L). Molecular docking studies also performed to understand the binding interaction.
- Morpholine hydrazones,
- Synthesis,
- HepG2,
- MCF-7,
- Molecular docking
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