片螺素D的D环缩合类似物的合成与生物学评价
Synthesis and biological evaluation of a D-ring-contracted analogue of lamellarin D.
作者信息
Colligs Vanessa, Hansen Steven Peter, Imbri Dennis, Seo Ean-Jeong, Kadioglu Onat, Efferth Thomas, Opatz Till
机构信息
Institute of Organic Chemistry, Johannes Gutenberg-University, Duesbergweg 10-14, 55128 Mainz, Germany.
Institute of Pharmacy and Biochemistry, Johannes Gutenberg-University, Staudinger Weg 5, 55128 Mainz, Germany.
出版信息
Bioorg Med Chem. 2017 Nov 15;25(22):6137-6148. doi: 10.1016/j.bmc.2017.02.005. Epub 2017 Feb 9.
A D-ring contracted analogue of the strongly cytotoxic marine pyrrole alkaloid lamellarin D was synthesized and investigated for its antiproliferative action towards a wild type and a multidrug resistant (MDR) cancer cell line. The compound was found to inhibit tumor cell growth at submicromolar concentrations and showed a lower relative resistance in the MDR cell line than the antitumor drug camptothecin to which lamellarin D shows cross resistance and with which lamellarin D shares the same binding site.
合成了具有强细胞毒性的海洋吡咯生物碱片螺素D的D环收缩类似物，并研究了其对野生型和多药耐药（MDR）癌细胞系的抗增殖作用。发现该化合物在亚微摩尔浓度下可抑制肿瘤细胞生长，并且在MDR细胞系中的相对耐药性低于抗肿瘤药物喜树碱，片螺素D对喜树碱表现出交叉耐药性，且与喜树碱共享相同的结合位点。
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