首页|Synthesis of Anti-Pancreatic Cancer Natural Product Majusculamide D and Analogues Reveals a Preliminary Structure-Activity Relationships

Synthesis of Anti-Pancreatic Cancer Natural Product Majusculamide D and Analogues Reveals a Preliminary Structure-Activity Relationships

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The total synthesis of majusculamide D(1)was achieved from commercially available materials.In addition,we synthesized eight an-alogues including three stereoisomers of majusculamide D that differ in the fatty acid chain.Six analogues including a simplified ana-logue 29 exhibited significant nanomolar-level IC50 values against Panc-1 cells in MTT assays.A preliminary SAR analysis indicated that the hydroxyl group at C1O and C2-C3 unsaturated double bond of majusculamide D were essential in maintaining the high activity against Panc-1 cells and the orientation of C40-Me and C42-Me groups was tolerable.

Majusculamide DNatural productsSARAnti-pancreatic cancerLipopentapeptide

Xiuhe Zhao、Mengxue Lv、Xiaonan Xi、Yaxin Lu、Liang Wang、Yue Chen

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The State Key Laboratory of Medicinal Chemical Biology,College of Pharmacy,Nankai University,Tianjin 300350,China

College of Chemistry,Nankai University,Tianjin 300071,China

国家自然科学基金国家自然科学基金中央高校基本科研业务费专项Hundred Young Academic Leaders Program of Nankai University(Nankai University)Frontiers Science Center for New Organic Matter

82073695U180128863181206

2024

10.1002/cjoc.202300526

中国化学(英文版)
中国化学会 上海有机化学研究所

中国化学(英文版)

CSTPCD
影响因子：0.848
ISSN：1001-604X
年,卷(期)：2024.42(6)
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