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Summary and Final Comments. In this study, we have identified three sets of biaoctive compounds based on the tricyclic core of the Stemona alkaloid skeleton shown in Fig. 6. These compounds vary in their degrees of added structural complexity from a simple amide reduction (6{10}) to a greater than twofold increase of the molecular weight via an isocyanide MCR (14{26}). Each of these compounds has provided potent binding compounds that may be viewed as lead structures for further development. Moreover, we identified a particular chemical feature consistent with activity (a basic nitrogen atom), which suggested a scaffold-hopping maneuver that resulted in unique compounds with exquisite potency and selectivity against the Sig-Rs. |
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8814402
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- Ó¦Öú: 18 (СѧÉú)
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- Ìû×Ó: 4183
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- ×¢²á: 2011-01-06
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2Â¥2011-07-20 10:07:44
8814402
ÖÁ×ðľ³æ (Ö°Òµ×÷¼Ò)
- ·ÒëEPI: 509
- Ó¦Öú: 18 (СѧÉú)
- ¹ó±ö: 0.381
- ½ð±Ò: 12916.1
- É¢½ð: 47
- ºì»¨: 16
- Ìû×Ó: 4183
- ÔÚÏß: 357.8Сʱ
- ³æºÅ: 1184404
- ×¢²á: 2011-01-06
- רҵ: Ò©ÎïѧÆäËû¿ÆÑ§ÎÊÌâ
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liugy2009(½ð±Ò+40, ·ÒëEPI+1): O(¡É_¡É)O~~~лл°ïæ 2011-07-20 19:19:34
Mally89(½ð±Ò+1): ¸ÐлӦÖú£¡~ 2011-07-23 22:02:26
liugy2009(½ð±Ò+40, ·ÒëEPI+1): O(¡É_¡É)O~~~лл°ïæ 2011-07-20 19:19:34
Mally89(½ð±Ò+1): ¸ÐлӦÖú£¡~ 2011-07-23 22:02:26
| Summary and Final Comments.×ܽáºÍ×îºóÆÀÂÛ In this study, we have identified three sets of biaoctive compounds based on the tricyclic core of the Stemona alkaloid skeleton shown in Fig. 6. ±¾Ñо¿ÖУ¬ÎÒÃǼø¶¨ÁË»ùÓÚË¹ÌæÄþ¼î¹Ç¼ÜÈý»·ºËÐĵÄÈý¸öϵÁеĻîÐÔ»¯ºÏÎ¼ûͼ6.These compounds vary in their degrees of added structural complexity from a simple amide reduction (6{10}) to a greater than twofold increase of the molecular weight via an isocyanide MCR (14{26}).ÕâЩ»¯ºÏÎïÔÚÔö¼ÓµÄ½á¹¹¸´ÔÓÐÔÉϸ÷²»Ïàͬ¡£ Each of these compounds has provided potent binding compounds that may be viewed as lead structures for further development. ÿÖÖϵÁл¯ºÏÎï¶¼¿ÉÑ¡³ö¿ÉÊÓ×÷½øÒ»²½¿ª·¢µÄÏȵ¼»¯ºÏÎïµÄ¸ßÇ׺ÍÐÔ»¯ºÏÎï¡£Moreover, we identified a particular chemical feature consistent with activity (a basic nitrogen atom), which suggested a scaffold-hopping maneuver that resulted in unique compounds with exquisite potency and selectivity against the Sig-Rs.¶øÇÒ£¬ÎÒÃÇ»¹¼ø¶¨ÁËÓë»îÐÔÒ»ÖµÄÒ»ÖÖÌØÊâµÄ»¯Ñ§ÌØÕ÷---¼îÐÔµªÔ×Ó£¬ÕâÌáʾ֧¼Ü±ä»»²ßÂԿɵõ½¶ÔSig-R¾ßÓÐÇ¿ÁÒ»îÐÔºÍÁéÃôÑ¡ÔñÐԵĶÀÌØ»¯ºÏÎï¡£ |
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