Benzoic acid, 3-[4-[[[3,4-dihydro-6-methyl-4-oxo-3-(phenylmethyl)-2-quinazolinyl]thio]methyl]-1H-1,2,3-triazol-1-yl]-

Uses

HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway[1].

IC 50

HSP90: 25.07 nM (IC₅₀); Topoisomerase-2: 25.85 nM (IC₅₀); EGFR: 38.5 nM (IC₅₀); VEGFR-2: 126.95 nM (IC₅₀)

References

[1] El-Shafey HW, et al. Synthetic approaches, anticancer potential, HSP90 inhibition, multitarget evaluation, molecular modeling and apoptosis mechanistic study of thioquinazolinone skeleton: Promising antibreast cancer agent. Bioorg Chem. 2020 Aug;101:10398 DOI:10.1016/j.bioorg.2020.103987