ChemInform Abstract: The Oxetane Ring in Taxol.
Abstract
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ChemInform Abstract
The oxetane ring of anticancer drug taxol (I) is regarded to be essential for the biological activity of the title compound. Computer-aided investigation of the structure—activity relationship ascertains the fact that it is not necessary, at least as it pertains to microtubule assembly, as supported by studies of oxetane heteroatom replacement, transformation of the oxetane into a three-membered ring, and transformation of taxol into D- or C-seco analogues. Thus, further optimization is of interest and will lead to the design and development of novel anticancer drugs.
