Related Experiment Video
Updated: Aug 29, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and Biological Evaluation of Thiazole-based Fibroblast Growth Factor Receptor-1 Inhibitors
Mohammad A Khanfar1,2, Ibrahim M Salman1, Omar Z Ameer1
1Department of Pharmaceutical Sciences, College of Pharmacy, Alfaisal University, Al Takhassusi Rd, Riyadh 11533, Saudi Arabia.
Background:
The Fibroblast Growth Factor Receptor-1 (FGFR-1) is a tyrosine kinase and a validated target for the treatment of different cancer types.
Objective:
Design and synthesis of novel thiazole-based analogues of anticancer agents.
Methods:
Series of 2-aryl-5-methylthiazole analogues linked to structurally variable basic heads were synthesized as novel anticancer agents. Developed compounds were tested for their cytotoxic activities against several cancer cell lines.
Results:
Many analogues exhibited strong antiproliferative activities against breast cancer cell lines, with higher potency towards the highly metastatic form (MDA-MB-231). Pharmacophoric profiling using an in-house pharmacophore database identified FGFR-1 as a molecular target of active analogues. Synthesized compounds were bioassayed for their FGFR-1 inhibitory activities and many hits exhibited IC50 values in the low micromolar to nanomolar range.
Conclusion:
The 2-aryl-5-methylthiazole linked to a basic head is a novel chemical scaffold of ATP-competitive inhibitor of FGFR-1 with potential therapeutic activities against different types of cancer.
More Related Videos
Related Concept Videos
Mitogens and the Cell Cycle
TGF - β Signaling Pathway
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Introduction to Fibroblasts

