AI Article Synopsis
- The study focused on understanding how modifications to the 7-hydroxyl groups of certain taxoid compounds affect their activity.
- Different modifications were tested, including deoxy, methoxy, alpha-fluorine, and a unique methano group.
- The 7-deoxy analogue was found to be the most potent, with stronger effects against specific cancer cell lines compared to related compounds.
Article Abstract
To investigate structure-activity relationships of the 9,10-acetal-9beta-dihydro taxoids, we modified the 7-hydroxyl groups of the 9,10-acetonide-3'-(4-pyridyl) analogue to deoxy, methoxy, alpha-F, and 7beta,8beta-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.
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| http://dx.doi.org/10.1016/s0960-894x(02)00628-5 | DOI Listing |
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