Synthesis, Characterization and Mechanistic Anticancer Evaluation of Novel Analogues of Pyrazoles Derived from Substituted 3-Acetyl Coumarins.
Aravinda Pai1*, Pooja Sharma P. C2, Venkatesh Kamath3, Chandrashekhar K. S4, Vasudev Pai5 and Muddukrishna B. S61Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India.
3Department of Pharmaceutical Biotechnology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India.
4Department of Pharmacognosy, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India.
6Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India
Corresponding Author E-mail: aravind.pai@manipal.edu
Abstract: In the present study, a congeneric series of novel substituted coumarin pyrazole carbaldehydes were synthesized. The compounds were characterized by various physical and spectroscopic methods. Preliminary cytotoxicity of the analogues was carried out using the MTT assay method on A-549 Lung cancer cell lines. The synthesized compounds possessed appreciable cytotoxicity against lung cancer cell lines. Out of the 8 synthesized compounds, the compound P-03 showed marked cytotoxicity of 13.5 mmol compared to standard doxorubicin which showed cytotoxicity value of 3.5 mmol. The compound P-03 was further investigated for its ability to induce apoptosis and its effect on cell cycle analysis. The compound P-03 was found to be an early apoptotic agent. After performing a cell cycle investigation, it was discovered that the compound P-03 effectively inhibited the G2/M phase of the cell cycle.
Keywords: Anticancer; Apoptosis; Coumarin; Cell Cycle; Hybrid; Mechanistic; Pyrazole Back to TOC