Related Experiment Video
Updated: Apr 28, 2026

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
Synthesis of Marine-Inspired Multifaceted DNA Damaging Spirooxindoles Combating NSCLC and Associated Bacterial
Mohammad Shahidul Islam1, Assem Barakat1, Abdul Majeed Abdullah Alayyaf1
1Department of Chemistry, College of Science, King Saud University, P. O. Box 2455, Riyadh 11451, Saudi Arabia.
None:
Targeted therapeutics have gained prominence in combating non-small cell lung carcinoma (NSCLC) and opportunistic bacterial infections like Staphylococcus aureus (S. aureus). This study explores dual-acting marine-inspired spirooxindoles to limit NSCLC and opportunistic bacteria. Pharmacophoric motifs from antitumor and antibacterial marine products were merged into a new series of pyrazole-clubbed spirooxindoles via a stereoselective [3 + 2] cycloaddition reaction. MTT screening identified 4e, 4i, and 4p-4s as potent cytotoxic agents, with 4p showing exceptional activity (IC50 = 0.042 μM) and tumor selectivity (SI = 58.28). 4p exhibited antibacterial efficacy against S. aureus (MIC = 25 μg/mL). DNA damage studies using a terbium(III) chloride biosensor revealed 4p's ability to damage both calf thymus and S. aureus DNA at low concentrations. Docking simulations presumed that 4p binds between DNA strands, while apoptosis studies indicated it induced G1/S phase cell cycle arrest and increased A549 apoptosis by 33.65%. These findings highlight 4p as a promising lead for further studies.
Related Concept Videos
Combined Effects of Drugs: Synergism
Such synergistic combinations...
Gene Regulation in Microbial Communities: Quorum Sensing
Inhibitors of Gram-positive Cell Wall Synthesis
Inhibitors of Bacterial Protein Synthesis
Inhibitors of Bacterial DNA Synthesis
Clinical Significance of Antibiotic Resistance

