Safety of Indolin-2-one. Recently I am researching about PLASMODIUM-FALCIPARUM M1; ACUTE NONLYMPHOCYTIC LEUKEMIA; MOLECULAR-DYNAMICS; CLINICAL-SIGNIFICANCE; EFFICIENT GENERATION; STRUCTURAL BASIS; AM1-BCC MODEL; CD13; BESTATIN; CANCER, Saw an article supported by the National Health and Medical Research CouncilNational Health and Medical Research Council of Australia [1063786]; Monash UniversityMonash University; Sir James McNeil Foundation; Cancer Therapeutics CRC, CTx. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Lee, J; Vinh, NB; Drinkwater, N; Yang, W; Sivaraman, KK; Schembri, LS; Gazdik, M; Grin, PM; Butler, GS; Overall, CM; Charman, SA; McGowan, S; Scammells, PJ. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one
Aminopeptidase N (APN/CD13) is a zinc-dependent M1 aminopeptidase that contributes to cancer progression by promoting angiogenesis, metastasis, and tumor invasion. We have previously identified hydroxamic acid-containing analogues that are potent inhibitors of the APN homologue from the malarial parasite Plasmodium falciparum M1 aminopeptidase (PfA-M1). Herein, we describe the rationale that underpins the repurposing of PfA-MI inhibitors as novel APN inhibitors. A series of novel hydroxamic acid analogues were developed using a structure-based design approach and evaluated their inhibition activities against APN. N-(2-(Hydroxyamino)-2-oxo-1-(3′,4′,5′-trifluoro-[1,1′-biphenyl]-4-yOethyl)-4(methylsulfonamido)benzamide (6ad) proved to be an extremely potent inhibitor of APN activity in vitro, selective against other zinc-dependent enzymes such as matrix metalloproteases, and possessed limited cytotoxicity against Ad293 cells and favorable physicochemical and metabolic stability properties. The combined results indicate that compound 6ad may be a useful lead for the development of anticancer agents.
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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem