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In addition to the scaffold bearing the ethyl side chain of stenine and neostenine, a collection of nonnatural Stemonalike ketoamide scaffolds were constructed via this route, which then served as the substrates for the preparation of six sets of functionalized analogues. These bore core changes that could not be readily accomplished by modification of the natural product itself. Representative examples of the various pathways of these initial efforts are shown in Scheme 2. Almost exclusively, these analogues displayed ring systems or functional groups substantially different from those of the natural products, including carbamates, amides, aryl groups, and heterocyclic moieties (e.g., indole and quinoline) (39). At the outset, it was unknown whether these analogues would possess any significant binding activity. |
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- ºì»¨: 16
- Ìû×Ó: 4183
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| In addition to the scaffold bearing the ethyl side chain of stenine and neostenine, a collection of nonnatural Stemonalike ketoamide scaffolds were constructed via this route, which then served as the substrates for the preparation of six sets of functionalized analogues. ³ýÁË´øÓÐË¹ÌæÄþ¼îºÍÐÂË¹ÌæÄþ¼îµÄÒÒÍé»ù²àÁ´µÄÖ§¼Ü£¬Ò»ÏµÁзÇÌìÈ»°Ù²¿Ñù°±»ù֧ͪ¼Üͨ¹ýÕâһ·Ïß¹¹½¨¡£These bore core changes that could not be readily accomplished by modification of the natural product itself. Õâ²úÉúµÄºËÐı仯²»Ò×ÓÚͨ¹ý¶ÔÌìÈ»²úÎï×ÔÉíµÄÐÞÊζøÊµÏÖ¡£Representative examples of the various pathways of these initial efforts are shown in Scheme 2. ÕâЩ¿ª´´ÐÔŬÁ¦µÄ²»Í¬Â·¾¶µÄ´ú±íÐÔÀý×ÓÏÔʾÓÚʾÒâͼ2ÖС£Almost exclusively, these analogues displayed ring systems or functional groups substantially different from those of the natural products, including carbamates, amides, aryl groups, and heterocyclic moieties (e.g., indole and quinoline) (39). ¼¸ºõÊÇÎÞÒ»ÀýÍâµÄ£¬ÕâЩÀàËÆÎï¶¼ÏÔʾÁËÓëÌìÈ»²úÎïÏ൱²»Í¬µÄ»·ÏµÍ³ºÍ¹ÙÄÜÍÅ£¬°üÀ¨°±»ù¼×Ëá¡¢õ£°·¡¢·¼»ù¼¯Íź;ֲ¿ÔÓ»·½á¹¹£¨ÈçßÅßáºÍàßø£©¡£At the outset, it was unknown whether these analogues would possess any significant binding activity.Æð³õ£¬ÕâЩÀàËÆÎïÊÇ·ñ¾ßÓÐÓÐЧµÄ½áºÏ»îÐÔÉв»µÃ¶øÖª¡£ |
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