186668-54-2Relevant academic research and scientific papers
Homocamptothecins: Synthesis and antitumor activity of novel E-ring- modified camptothecin analogues
Lavergne, Olivier,Lesueur-Ginot, Laurence,Rodas, Francesc Pla,Kasprzyk, Philip G.,Pommier, Jacques,Demarquay, Danièle,Prévost, Grégoire,Ulibarri, Gérard,Rolland, Alain,Schiano-Liberatore, Anne-Marie,Harnett, Jeremiah,Pons, Dominique,Camara, José,Bigg, Dennis C. H.
, p. 5410 - 5419 (1998)
Homocamptothecin (hCPT), a camptothecin (CPT) analogue with a seven membered β-hydroxylactone which combines enhanced plasma stability and potent topoisomerase I (Topo I) mediated activity, is an attractive template for the elaboration of new anticancer a
Practical racemic and asymmetric formal total syntheses of the homocamptothecin derivative and anticancer agent diflomotecan via tertiary homoallylic alcohols as masked aldol equivalents
Peters, Rene,Diolez, Christian,Rolland, Alain,Manginot, Eric,Veyrat, Marc
, p. 255 - 273 (2008/03/12)
An efficient and scalable racemic as well as an asymmetric approach to the key building block for the synthesis of homocamptothecin and derivatives thereof such as the potent anticancer agent diflomotecan (4) are described. In the asymmetric route, the pyridone ring was assembled applying straightforward carbonyl chemistry. The selective generation of the quaternary stereocenter was accomplished by self reproduction of chiral information starting from (S)-2-hydroxybutyric acid (22) utilizing an allyl moiety to act as a masked carbonyl group. The optically pure DE building block (7) (er > 99.95 : 0.05) was obtained in 9.0% overall yield over 10 steps (two chromatographic purifications). The asymmetric "de novo pyridone approach" has the potential to serve as the basis for a technical synthesis of diflomotecan.
Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
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, (2008/06/13)
A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
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, (2008/06/13)
A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
Comptothecin analogues, preparation methods therefor, use thereof as drugs, and pharmaceutical compositions containing said analogues
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Example 11, (2008/06/13)
The compound of the formula wherein the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable salts which are useful for the treatment of viral infections, parasitic diseases and the treatment of cancer.
