Ribeiro, Carlos J. A. published the artcileTriazolopyrimidine and triazolopyridine scaffolds as TDP2 inhibitors, Name: 3,5-Diamino-1,2,4-triazole, the main research area is TDP2 inhibitors anticancer triazolo pyrimidines pyridines SAR; Anti-cancer; Triazolo-pyridines; Triazolo-pyrimidines; Tyrosyl-DNA phosphodiesterase 2 (TDP2).
Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (TOP2) mediated DNA damages and causes cellular resistance to clin. used TOP2 poisons. Inhibiting TDP2 can potentially sensitize cancer cells toward TOP2 poisons. Com. compound P10A10, to which the structure was assigned as 7-Ph triazolopyrimidine analog 6a, was previously identified as a TDP2 inhibitor hit in our virtual and fluorescence-based biochem. screening campaign. We report herein that the hit validation through resynthesis and structure elucidation revealed the correct structure of P10A10 (Chembridge ID 7236827) to be the 5-Ph triazolopyrimidine regioisomer 7a. Subsequent structure-activity relationship (SAR) via the synthesis of a total of 47 analogs of both the 5-Ph triazolopyrimidine scaffold (7) and its bioisosteric triazolopyridine scaffold (17) identified four derivatives (7a, 17a, 17e, and 17z) with significant TDP2 inhibition (IC50 < 50 μM), with 17z(I) showing excellent cell permeability and no cytotoxicity. Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents (sensitize cancer cells). 1455-77-2 belongs to class isoquinoline, name is 3,5-Diamino-1,2,4-triazole, and the molecular formula is C2H5N5, Name: 3,5-Diamino-1,2,4-triazole.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem