160237-44-5Relevant academic research and scientific papers
Design, synthesis and structure-activity relationships of novel taxane-based multidrug resistance reversal agents
Ojima, Iwao,Borella, Christopher P.,Wu, Xinyuan,Bounaud, Pierre-Yves,Oderda, Cecilia Fumero,Sturm, Matthew,Miller, Michael L.,Chakravarty, Subrata,Chen, Jin,Huang, Qing,Pera, Paula,Brooks, Tracy A.,Baer, Maria R.,Bernacki, Ralph J.
, p. 2218 - 2228 (2007/10/03)
A series of novel taxane-based multidrug resistance (MDR) reversal agents (TRAs) has been designed and synthesized. Structure - activity relationship (SAR) study clearly indicates that modification of the C-7 position with hydrophobic arenecarbonylcinnamoyl groups brings about high potency against drug efflux mediated by P-glycoprotein (P-gp). Six TRAs exhibit ability to modulate a wide range of ATP-binding cassette (ABC) transporters, such as P-gp, multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein (BCRP), which may serve as novel broad-spectrum modulators of ABC transporters.
New highly active taxoids from 9β-dihydrobaccatin-9,10-acetals. Part 2
Ishiyama, Takashi,Iimura, Shin,Yoshino, Toshiharu,Chiba, Jun,Uoto, Kouichi,Terasawa, Hirofumi,Soga, Tsunehiko
, p. 2815 - 2819 (2007/10/03)
To investigate structure-activity relationships of the 9,10-acetal-9β-dihydro taxoids, we modified the 7-hydroxyl groups of the 9,10-acetonide-3′-(4-pyridyl) analogue to deoxy, methoxy, α-F, and 7β,8β-methano group. As a result of this study, we found that the 7-deoxy analogue was the strongest among these analogues. In addition, we found that the 7-deoxy-3′-(4-pyridyl) and 7-deoxy-3′-(2-pyridyl) analogues showed stronger activity against cell lines expressing P-glycoprotein than the corresponding 3′-phenyl analogue.
A semisynthesis of paclitaxel via a 10-deacetylbaccatin III derivative bearing a β-keto ester appendage
Mandai, Tadakatsu,Kuroda, Akiyoshi,Okumoto, Hiroshi,Nakanishi, Katsuyoshi,Mikuni, Katsuhiko,Hara, Ko-Ji,Hara, Ko-Zo
, p. 243 - 246 (2007/10/03)
A semisynthesis of paclitaxel has successfully been accomplished starting from a newly developed baccatin III derivative bearing a β-keto ester appendage on C-13.
