Abstract
Taxol, isolated from the bark of Taxus breVifolia in the late 1960s, 1 and its semisynthetic Taxotere congener 2 have become the drugs of choice for the treatment of ovarian and breast cancer. 3 The availability of active simplified analogues would facilitate shortened synthetic strategies and potentially bypass neurotoxicity 4 and multidrug resistance. 5 The design of such compounds is hampered by an incomplete understanding of Taxol’s conformation in the bioactive form. Numerous studies have sought to deduce the drug’s three-dimensional state in solution by NMR spectroscopy combined with force-field guided conformational analysis. In both polar and nonpolar solvents, rotamers exhibit hydrophobic collapse 6 between the flexible C-2, C-4, and C-13 side chains, accompanied by variable H2′-C-C-H3′ torsional angles (Table 1). 7,8 Each of the conformational extremes has been proposed as a candidate for the Taxol topology bound to microtubules. 7d,g-j,8b-d
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
