Synthesis, anticancer and antimicrobial evaluation of new pyridyl and thiazolyl clubbed hydrazone scaffolds

Abstract

A series of new hydrazones bearing pyridyl and thiazolyl scaffolds have been synthesized and evaluated for their in vitro anticancer and antimicrobial activities. The anticancer activity was evaluated against the A549 lung cancer cell line. The eight hydrazone derivatives have shown better anticancer activity than positive control doxorubicin against the A549 lung cancer cell line. The antimicrobial activity was evaluated against bacterial and fungal pathogens by using well diffusion method. The four hydrazone derivatives have displayed good antimicrobial activities. Molecular docking studies of the synthesized hydrazone derivatives revealed good binding via hydrogen bond interactions with key residues on active sites as well as neighboring residues with an active site of Focal adhesion kinase (PDB ID 2JKO). A computational study for the prediction of absorption, distribution, metabolism, and excretion (ADME) properties of all compounds has also been performed.

Graphical Abstract

Keywords:

• Anticancer activity
• antimicrobial activity
• thiazoles
• hydrazones
• molecular docking study
• ADME prediction

Acknowledgment

Authors are thankful to Prof. R. A. Mane for their guidance and valuable discussions. We are also thankful to Dr. Babasaheb Ambedkar Marathwada University Aurangabad for financial assistance (File No. STAT/V1/RG/Dept/2019-20/323-324).

Additional information

Funding

This work was supported by Dr. Babasaheb Ambedkar Marathwada University Aurangabad for financial assistance.