ChemInform Abstract: DNA Topoisomerase I Inhibitors: Chemistry, Biology, and Interfacial Inhibition

ChemInform ◽  
2009 ◽  
Vol 40 (46) ◽  
Author(s):  
Yves Pommier
2011 ◽  
Vol 64 (10) ◽  
pp. 1390 ◽  
Author(s):  
Ling-Jian Zhu ◽  
Chun-Lin Zhuang ◽  
Ning Lei ◽  
Chun-Quan Sheng ◽  
Wei Guo ◽  
...  

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.


Author(s):  
Tatsuo Ohira ◽  
Kazuto Nishio ◽  
Fumihiko Kanzawa ◽  
Tomoyuki Ishida ◽  
Yuichiro Ohe ◽  
...  

1995 ◽  
Vol 38 (6) ◽  
pp. 906-911 ◽  
Author(s):  
Karen Lackey ◽  
Jeffrey M. Besterman ◽  
Wade Fletcher ◽  
Peter Leitner ◽  
Bradley Morton ◽  
...  

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