186668-40-6Relevant articles and documents
BN 80245: An E-ring modified camptothecin with potent antiproliferative and topoisomerase I inhibitory activities
Lavergne, Olivier,Lesueur-Ginot, Laurence,Rodas, Francesc Pla,Bigg, Dennis C. H.
, p. 2235 - 2238 (1997)
The crucial E-ring of camptothecin has been modified to afford the homologous β-hydroxylactone derivative BN 80245. This compound, which is more stable than camptothecin, remains a potent inhibitor of both cell growth and topoisomerase I.
Synthesis and cytotoxicity of novel 20-O-linked homocamptothecin ester derivatives as potent topoisomerase I inhibitors
Li, Di-Zao,Wang, Cun-Ying,Liu, Rui-Hua,Wang, Yan-Ming,Ji, Teng-Fei,Li, Yu-Rong,Pan, Xian-Dao
, p. 1179 - 1188 (2014/01/06)
In an attempt to improve the antitumor activity of homocamptothecins (hCPTs), a series of novel 20-O-linked hCPT ester derivatives were first designed and synthesized based on a synthetic route, by which hCPTs are acylated with different substituted pheno
New homocamptothecins: Synthesis, antitumor activity, and molecular modeling
Miao, Zhenyuan,Sheng, Chunquan,Zhang, Wannian,Ji, Haitao,Zhang, Jing,Shao, Luecheng,You, Liang,Zhang, Min,Yao, Jianzhong,Che, Xiaoyin
, p. 1493 - 1510 (2008/09/17)
Homocamptothecins (hCPTs) represent a class of new emerging antitumor agents, which contains a seven-membered β-hydroxylactone in place of the conventional six-membered α-hydroxylactone ring (E ring) of camptothecins. Some novel 7-substituted hCPTs were designed and synthesized based on a newly developed synthetic route which couples ring A with ring C, E and D. Most of the synthesized compounds exhibit very high cytotoxic activity on tumor cell line A549. Some compounds, such as 9b, 9l, and 9y, show broad in vitro antitumor spectrum and are more potent than topotecan. Three-dimensional quantitative structure-activity relationship (3D-QSAR) methods, CoMFA and CoMSIA, were applied to explain the structure-activity relationship (SAR) of the synthesized compounds. Furthermore, molecular docking was used to clarify the binding mode of the synthesized compounds to human DNA topoisomerase I. The important hydrophobic, base-pair stacking, and hydrogen-bonding interactions were observed between the hCPT derivatives and their receptor. The results from molecular modeling will guide the design of novel hCPTs with higher antitumor activity.
Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
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, (2008/06/13)
A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
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, (2008/06/13)
A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
Comptothecin analogues, preparation methods therefor, use thereof as drugs, and pharmaceutical compositions containing said analogues
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Example 3, (2008/06/13)
The compound of the formula wherein the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable salts which are useful for the treatment of viral infections, parasitic diseases and the treatment of cancer.
Homocamptothecins: Synthesis and antitumor activity of novel E-ring- modified camptothecin analogues
Lavergne, Olivier,Lesueur-Ginot, Laurence,Rodas, Francesc Pla,Kasprzyk, Philip G.,Pommier, Jacques,Demarquay, Danièle,Prévost, Grégoire,Ulibarri, Gérard,Rolland, Alain,Schiano-Liberatore, Anne-Marie,Harnett, Jeremiah,Pons, Dominique,Camara, José,Bigg, Dennis C. H.
, p. 5410 - 5419 (2007/10/03)
Homocamptothecin (hCPT), a camptothecin (CPT) analogue with a seven membered β-hydroxylactone which combines enhanced plasma stability and potent topoisomerase I (Topo I) mediated activity, is an attractive template for the elaboration of new anticancer a
