1000000-06-5Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of novel homocamptothecin- dihydropyridine derivative conjugates as potent topoisomerase i inhibitors
Zhu, Ling-Jian,Zhuang, Chun-Lin,Lei, Ning,Sheng, Chun-Quan,Guo, Wei,Miao, Zhen-Yuan,Liu, Wen-Feng,Yao, Jian-Zhong,Zhang, Wan-Nian
, p. 1390 - 1396 (2011)
Homocamptothecins (hCPT) represent a new generation of antitumour agents targeting DNA topoisomerase I. The expanded seven-membered lactone E-ring that characterizes hCPT enhances the plasma stability of the drug and reinforces the inhibition of topoisomerase I (Topo I) compared with conventional six-membered CPT. In an attempt to improve the antitumour activity of hCP, a series of novel hCPT derivatives conjugating with dihydropyridine derivates were designed and synthesized based on a synthetic route that couples 7-formylhomocamptothecin with different dihydropyridine derivates. Most of the synthesized compounds exhibited good cytotoxic activity on tumour cell line A549, MDA-MB-435, and HCT116. Furthermore, this class of compounds showed superior Topo I inhibition activity comparable to or higher than CPT. CSIRO 2011.
