Synthesis and Biological Evaluation of Novel Macrocyclic Paclitaxel Analogues
العنوان: | Synthesis and Biological Evaluation of Novel Macrocyclic Paclitaxel Analogues |
---|---|
المؤلفون: | David G. I. Kingston, Ami Lakdawala, Jeannine Hoch, James P. Snyder, Susan Bane, Sabarni K. Chatterjee, Thomas E. Glass, Ben Cornett, Belhu B. Metaferia |
المصدر: | Organic Letters. 3:2461-2464 |
بيانات النشر: | American Chemical Society (ACS), 2001. |
سنة النشر: | 2001 |
مصطلحات موضوعية: | Models, Molecular, Binding Sites, Paclitaxel, Olefin metathesis, Chemistry, Stereochemistry, Electron crystallography, Organic Chemistry, Molecular Conformation, Crystallography, X-Ray, Antineoplastic Agents, Phytogenic, Biochemistry, Combinatorial chemistry, Taxoid, chemistry.chemical_compound, Cyclization, Tubulin, Tumor Cells, Cultured, Humans, Indicators and Reagents, Physical and Theoretical Chemistry, Binding site, Biological evaluation |
الوصف: | [reaction: see text] This work describes the synthesis of two novel macrocyclic taxoid constructs by ring-closing olefin metathesis (RCM) and their biological evaluation. Computational studies examine conformational profiles of 1 and 2 for their fit to the beta-tubulin binding site determined by electron crystallography. The results support the hypothesis that paclitaxel binds to microtubules in a "T" conformation. |
تدمد: | 1523-7052 1523-7060 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf05d9a6e5000433f701089fae85adf9 https://doi.org/10.1021/ol016124d |
رقم الأكسشن: | edsair.doi.dedup.....bf05d9a6e5000433f701089fae85adf9 |
قاعدة البيانات: | OpenAIRE |
تدمد: | 15237052 15237060 |
---|