160768-77-4Relevant academic research and scientific papers
Synthesis and biological evaluation of novel paclitaxel (Taxol) D-ring modified analogues
Gunatilaka, A. A. Leslie,Ramdayal, Frank D.,Sarragiotto, Maria H.,Kingston, David G. I.,Sackett, Dan L.,Hamel, Ernest
, p. 2694 - 2703 (2007/10/03)
The semisynthesis and biological activity of paclitaxel (Taxol) analogues in which the oxygen atom in ring D is substituted by a sulfur or a selenium atom is presented. These derivatives were synthesized and tested in order to make more transparent the role of the oxetane ring in the biological activity of paclitaxel. The sulfur derivatives were found to be less active than paclitaxel in biological assays, while the selenium derivative could not be converted to its 4-acyl analogue. The results with the sulfur analogues suggest that the oxygen atom in the oxetane ring plays an important role in the mechanism by which paclitaxel exhibits its anticancer activity.
Selective C-2 and C-4 deacylation and acylation of taxol: The first synthesis of a C-4 substituted taxol analogue
Georg,Georg, Gunda I.,Ali,Ali, Syed M.,Boge,Boge, Thomas C.,Datta,Datta, Apurba,Falborg,Falborg, Lise,Himes,Himes, Richard H.
, p. 8931 - 8934 (2007/10/02)
Hydrolytic procedures for selective 2-debenzoylation and 2,4-dideacylation of 2'-O-tert-butyldimethylsilyl-7-O-(triethylsilyl)taxol are reported. The first synthesis and biological evaluation of a 4-substituted analogue, 4-deacetyl-4-isobutanoyltaxol, is
Synthesis and Biological Evaluation of 4-Deacetoxypaclitaxel
Chordia, Mahendra D.,Chaudhary, Ashok G.,Kingston, David G. I.,Jiang, Yuan Qing,Hamel, Ernest
, p. 6843 - 6846 (2007/10/02)
4-Deacetoxypaclitaxel (9) has been prepared in seven steps from paclitaxel (Taxol).It is significantly less active than paclitaxel in tubulin-assembly and cytotoxicity bioassays.
