A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 4474-86-6, Name is N-Cbz-D-Asparagine, molecular formula is C12H14N2O5. In an article, author is Reilly, Sean W.,once mentioned of 4474-86-6, Safety of N-Cbz-D-Asparagine.
Development of poly(ADP-ribose) polymerase inhibitors (PARPi’s) continues to be an attractive area of research due to synthetic lethality in DNA repair deficient cancers; however, PARPi’s also have potential as therapeutics to prevent harmful inflammation. We investigated the pharmacological impact of incorporating spirodiamine motifs into the phthalazine architecture of FDA approved PARPi olaparib. Synthesized analogues were screened for PARP-1 affinity, enzyme specificity, catalytic inhibition, DNA damage, and cytotoxicity. This work led to the identification of 10e (12.6 +/- 1.1 nM), which did not induce DNA damage at similar drug concentrations as olaparib. Interestingly, several worst in class compounds with low PARP-1 affinity, including 15b (4397 +/- 1.1 nM), induced DNA damage at micromolar concentrations, which can explain the cytotoxicity observed in vitro. This work provides further evidence that high affinity PARPi’s can be developed without DNA damaging properties offering potential new drugs for treating inflammatory related diseases.
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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem