Design, synthesis, and evaluation of carbamate-substituted analogues of (+)-discodermolide |
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Authors: | Smith Amos B Freeze B Scott Lamarche Matthew J Hirose Tomoyasu Brouard Ignacio Rucker Paul V Xian Ming Sundermann Kurt F Shaw Simon J Burlingame Mark A Horwitz Susan Band Myles David C |
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Affiliation: | Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA. smithab@sas.upenn.edu |
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Abstract: | [Structure: see text] The design, syntheses, and biological evaluation of 22 totally synthetic analogues of the potent microtubule-stabilizing agent (+)-discodermolide (1) have been achieved. Structure-activity relationships of the C(19) carbamate were defined, exploiting two synthetically simplified scaffolds, as well as the parent (+)-discodermolide framework. |
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