A recent publication of our esteemed group titled (Multi-target rational design and synthesis of novel diphenyl-tethered pyrazolopyrimidines targeting EGFR and topoisomerase II with potential DNA intercalation and apoptosis induction) has been published in Bioorganic Chemistry, where:
?? Novel pyrazolopyrimidines were designed as multitarget-directed drug candidates.
?? GI % against fifteen human cancer cell lines was recorded.
?? Cytotoxicity against HNO97, MDA-MB-468, FaDu, and HeLa were measured.
?? Compound 6l decreased EGFR protein concentration by a 6.10-fold change, compared to imatinib.
?? Compounds 6a and 6l exhibited IC50 values of 17.89 and 19.39 μM, respectively, against TOPO II.
?? DNA fragmentation images described the great potential of 6a and 6l in inducing DNA degradation.
?? Protein expression analysis for caspases 3, 7, 8, and 9, Bax, p53, MMP2, MMP9, and BCL-2 was conducted.
?? Cell cycle analysis and molecular docking were performed.
Have an interesting reading with the nicely introduced rational design. Regards ??
#medicinalchemistry
#rational
#anticancer
Vice President of Business Development – Head of North America
1 个月Jim Mellon please introduce yourself to my colleagues from Mabion, who are also at the Festival of Biologics.