232920-75-1Relevant 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 photoaffinity analogs of paclitaxel
Ojima, Iwao,Bounaud, Pierre-Yves,Ahern, David G.
, p. 1189 - 1194 (2007/10/03)
Two new photoreactive paclitaxel analogs bearing [3H2]-3-(4- benzoyl)phenylpropanoyl group as the photophore as well as radiolabeling unit at the 7 and 10 positions, respectively, are developed. These new photoreactive analogs showed
New taxanes as highly efficient reversal agents for multidrug resistance in cancer cells
Ojima, Iwao,Bounaud, Pierre-Yves,Takeuchi, Craig,Pera, Paula,Bernacki, Ralph J.
, p. 189 - 194 (2007/10/03)
New non-cytotoxic taxanes synthesized from 10-deacetylbaccatin III and special hydrophobic acylating agents show remarkable MDR reversal activity (≤99.8%) against drug-resistant human breast cancer cells when co-administered with paclitaxel or doxorubicin. This activity is ascribed to the highly efficient blocking of P-glycoprotein efflux by these new taxanes.
