Bisantrene

  • Chemical Properties
CAS No. 78186-34-2 Cat. No. BCP20206
Name Bisantrene
Synonyms
Formula C22H22N8 M. Wt 398.46
  • Biological Activity
Description Bisantrene shows an outstanding ability to form a complex with DNA. Bisantrene exhibits the most effective binding (even neglecting electrostatic contacts), followed by the 9-substituted compounds and finally by 1-IHA. Bisantrene congeners retained a remarkable capacity for binding to the single-stranded structure. In comparison with the Ki values found for double-stranded DNA, 9-IHA shows a 2-fold increase, 1-IHA maintains the same values, and aza-9-IHA exhibits a modest reduction. On the other hand, Bisantrene, although undergoing a 6-fold reduction in Ki, still exhibits an affinity constant of the order of 106 M-1. Bisantrene promots DNase I cleavage at oligopurine-oligopyrimidine tracts; conversely, it slightly reduces the cleavage activity at alternating purine-pyrimidine sequences. Bisantrene is an active new drug in the treatment of metastatic breast cancer. Bisantrene is an inhibitor of [3H]uridine incorporation into RNA and [3H]thymidine incorporation into DNA.
Related Products 71439-68-4(Bisantrene dihydrochloride)
Pathways Cell Cycle/DNA Damage 
Targets Topoisomerase 

Structure

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