Dallavalle Sabrina, Merlini Lucio, Beretta Giovanni Luca, Tinelli Stella, Zunino Franco
Dipartimento di Scienze Molecolari Agroalimentari, Sezione di Chimica, Università di Milano, Via Celoria 2, 20133 Milano, Italy.
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5757-61. doi: 10.1016/j.bmcl.2004.09.039.
Luotonin A is a cytotoxic alkaloid that has been shown to inhibit topoisomerase I via stabilization of the binary complex topoisomerase-DNA in the same fashion as camptothecin. The synthesis and the cytotoxic activity on the lung carcinoma cell line H460 of a series of derivatives of Luotonin A is reported. The compounds inhibit topoisomerase I but show weak cytotoxic activity, thus confirming the peculiarity of ring E of camptothecin for antitumor activity.
路脱辛A是一种细胞毒性生物碱，已证明它能以与喜树碱相同的方式通过稳定拓扑异构酶-DNA二元复合物来抑制拓扑异构酶I。本文报道了一系列路脱辛A衍生物的合成及其对肺癌细胞系H460的细胞毒性活性。这些化合物能抑制拓扑异构酶I，但细胞毒性活性较弱，从而证实了喜树碱E环在抗肿瘤活性方面的独特性。
