A one-pot, efficient synthesis of the potent cytotoxic podophyllotoxin derivative NPF
One-pot syntheses of 4'-demethylepipodophyllotoxin 7 and NPF 2 (4'-O-demethyl-4β-(4'-fluoroanilino )-4-deoxypodaphyllotoxin) are described from podophyllotoxin 3 via a protocol using trimethylsilyl iodide in 72% and 52% overall yields, respectively.
Daley, Laurent,Meresse, Philippe,Bertounesque, Emmanuel,Monneret, Claude
A one-pot, efficient and facile synthesis of 4β -arylaminopodophyllotoxins: Synthesis of NPF and GL-331 as DNA topoisomerase II inhibitors
A series of 4β-arylamino-4′-O-demethylepipodophyllotoxins and 4β-arylaminopodophyllotoxins have been synthesized with significant stereoselectivity and improved yields by employing the BF3· OEt2/NaI reagent system. Compounds NPF, GL-331 and other DNA topoisomerase II inhibitors have been prepared in good to excellent yields by employing this methodology.
Kamal, Ahmed,Kumar, B. Ashwini,Arifuddin
p. 8457 - 8459
(2007/10/03)
Facile and efficient one-pot synthesis of 4β-arylamino-podophyllotoxins: Synthesis of DNA topoisomerase II inhibitors (NPF and W-68)
A series of 4β-arylamino-4'-O-demethylepipodophyllotoxins and 4β-arylaminoepipodophyllotoxins have been synthesized with significant stereoselectivity and improved yields by employing the methanesulphonic acid/sodium iodide reagent system. Compounds NPF, W-68 and other DNA topoisomerase II inhibitors are prepared in good to excellent yields by this method and these are active or more active than etoposide in their inhibition of the human DNA topoisomerase II. (C) 2000 Elsevier Science Ltd.
Kamal, Ahmed,Laxman,Ramesh
p. 2059 - 2062
(2007/10/03)
An efficient method for 4β-anilino-4'-demethylepipodophyllotoxins: Synthesis of NPF and W-68
4β-Substituted podophyllotoxin congeners have been obtained with significant stereoselectivity and improved yields by employing Bu4N+I in the displacement reaction of the 4-bromoepipodophyllotoxin. The DNA topoisomerase II inhibitors, NPF and W-68 have been prepared in good yields by this method.
Kamal,Gayatri
p. 3359 - 3362
(2007/10/03)
Antitumor agents. 144. New γ-lactone ring-modified arylamino etoposide analogs as inhibitors of human DNA topoisomerase II
The trans-fused γ-lactone ring of etoposide is readily epimerized to its cis epimer, which is biologically inactive, or is metabolized to the inactive ring-opened hydroxy acids. Modification of this γ-lactone ring of 4β- (arylamino)-4'-O-demethyl-4-desoxy
Zhou,Lee,Cheng,Wu,Chen,Guo,Cheng -,Lee
p. 287 - 292
(2007/10/02)
Antitumor Agents. 111. New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II
A series of C-4 hydroxylated and halogenated anilino derivatives of epipodophyllotoxin or 4'-demethylepipodophyllotoxin have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity
Lee, Kuo-Hsiung,Beers, Scott A.,Mori, Masami,Wang, Zhe-Qing,Kuo, Yao-Haur,et al.
p. 1364 - 1368
(2007/10/02)
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