Synthesis and biological assays of E-ring analogs of camptothecin and homocamptothecin.
Synthesis and biological assays of E-ring analogs of camptothecin and homocamptothecin.
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DOI：
10.1016/j.bmc.2006.05.073
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发表时间：
2006-09
影响因子：
3.5
通讯作者：
Raghuram S. Tangirala;Smitha Antony;K. Agama;Y. Pommier;B. D. Anderson;Robert L. Bevins;D. Curran
中科院分区：
文献类型：
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作者：
Raghuram S. Tangirala;Smitha Antony;K. Agama;Y. Pommier;B. D. Anderson;Robert L. Bevins;D. Curran
已制备具有闭合E-环（内酯和醚）和开放E-环（还原酸、酰肼和保护的Weinreb酰胺）的抗肿瘤剂喜树碱的类似物，并在拓扑异构酶和细胞测定中进行测试。这些结果提供了对影响生物活性的喜树碱E环的结构特征的见解。
Analogs of the anti-tumor agent camptothecin with both closed E-rings (lactone and ether) and open E-rings (reduced acid, hydrazide, and protected Weinreb amide) have been prepared and tested in topoisomerase and cellular assays. The results provide insights into the structural features of the camptothecin E-ring that affect biological activity.