Synthesis of novel pyrazolines for subsequent structure-activity relationship study as inhibitors of microtubule polymerization
During the process of mitosis, microtubules form the structures the spindle fibers. These highly dynamic filamentous structures are among the most validated cancer targets. Compounds with heterocyclic pyrazoline rings are widely present in various natural products and are known to possess anti-tumor, anti-angiogenic and anti-inflammatory properties. In a recent work, we showed that these compounds are capable of modulating the microtubule dynamics. The work led to identification of novel hit with GI50 value of 197 ± 0.05 nM. In the current work, we are interested in developing several novel pyrazoline derivatives for subsequent structure activity relationship study as polymerization inhibitors.
- Dr. Rahman Shah Zaib Saleem (supervisor)
- Dr. Basit Yameen (thesis committee member)
- Dr. Ghayoor Abbas Chotana (thesis committee member)