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Anticancer properties of an important drug lead podophyllotoxin can be efficiently mimicked by diverse heterocyclic scaffolds accessible via one-step synthesis.

Abstract：

:Structural simplification of an antimitotic natural product podophyllotoxin with mimetic heterocyclic scaffolds constructed using multicomponent reactions led to the identification of compounds exhibiting low nanomolar antiproliferative and apoptosis-inducing properties. The most potent compounds were found in the dihydropyridopyrazole, dihydropyridonaphthalene, dihydropyridoindole, and dihydropyridopyrimidine scaffold series. Biochemical mechanistic studies performed with dihydropyridopyrazole compounds showed that these heterocycles inhibit in vitro tubulin polymerization and disrupt the formation of mitotic spindles in dividing cells at low nanomolar concentrations, in a manner similar to podophyllotoxin itself. Separation of a racemic dihydropyridonaphthalene into individual enantiomers demonstrated that only the optical antipode matching the absolute configuration of podophyllotoxin possessed potent anticancer activity. Computer modeling, performed using the podophyllotoxin binding site on β-tubulin, provided a theoretical understanding of these successful experimental findings.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Magedov IV,Frolova L,Manpadi M,Bhoga Ud,Tang H,Evdokimov NM,George O,Georgiou KH,Renner S,Getlik M,Kinnibrugh TL,Fernandes MA,Van slambrouck S,Steelant WF,Shuster CB,Rogelj S,van Otterlo WA,Kornienko A

doi

10.1021/jm200410r

subject

Has Abstract

pub_date

2011-06-23 00:00:00

pages

4234-46

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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