首页|Synthesis and Cytotoxic Activity of Fingolimod (FTY720) Analogs with Various Amide Head Groups

Synthesis and Cytotoxic Activity of Fingolimod (FTY720) Analogs with Various Amide Head Groups

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A series of 30 new analogs maintaining the backbone structure of FTY720 were synthesized by a very simple method. Regardless of newly introduced aromatic and non-aromatic head groups, the obtained structures showed cytotoxic effects. Specifically, in the case of aromatic head structures, only the head group containing nitrogen showed cytotoxic effects. In the case of non-aromatic head group, compound 23 with a relatively long chain head group showed this effect even at low concentrations. All the cytotoxic compounds showed protein phosphatase 2A activity and apoptotic effects regardless of the sphingosine kinase 1/2 inhibitory effect. Therefore, it was confirmed that the FTY720 backbone structure was an important factor that activated PP2A, resulting in anticancer effects.

sphingosine-1-phosphateanticancerFTY720protein phosphatase 2AderivativesSPHINGOSINEINHIBITORSMETABOLISMPOTENTCELLS

Kim, Su Bin、Kim, Kwang Joon、Shrestha, Jitendra、Oh, Yoon Sin、Lee, Joo-Youn、Lee, Seungyeon、Park, Eun-Young、Baek, Dong Jae

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Coll Pharm,Mokpo Natl Univ

Dept Food Nutr,Eulji Univ

Therapeut & Biotechnol Div,Korea Res Inst Chem Technol

New Drug Dev Ctr,Daegu Gyeongbuk Med Innovat Fdn

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2022

Pharmaceutical Chemistry Journal

Pharmaceutical Chemistry Journal

SCI
ISSN:0091-150X
年,卷(期):2022.56(4)
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