Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
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通过格氏反应在 7 位具有庞大的疏水取代基的喜树碱类似物。
DOI:
10.1016/j.bmcl.2004.08.010
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发表时间:
2004
期刊:
影响因子:
--
通讯作者:
Wall,MonroeE
中科院分区:
文献类型:
--
作者:
Manikumar,Govindarajan;Wadkins,RandyM;Bearss,David;VonHoff,DanielD;Wani,MansukhlalC;Wall,MonroeE
By developing a new synthetic procedure for introduction of side chains onto the camptothecin ring system, we were able to achieve the preparation of a number of analogs bearing bulky, hydrophobic groups directly attached to the 7-position. These include 7-tert-butylcamptothecin, 7-benzylcamptothecin and the corresponding 10,11-methylenedioxycamptothecins. This method involves the reaction of an appropriate orthoaminobenzonitrile with various Grignard reagents to give the corresponding orthoaminoketones. Friedlander condensation of the latter with the key tricyclic ketone leads to 7-substituted camptothecin analogs. We report the activity of these compounds as topoisomerase I poisons and their ability to inhibit growth of selected tumor cell lines.
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影响因子:
7.3
作者:
M. Wani;A. W. Nicholas;G. Manikumar;Monroe E. Wall
通讯作者:
M. Wani;A. W. Nicholas;G. Manikumar;Monroe E. Wall
影响因子:
11.2
作者:
Y. Hsiang;M. G. Lihou;Leroy F. Liu
通讯作者:
Y. Hsiang;M. G. Lihou;Leroy F. Liu
影响因子:
8.4
作者:
Francés-Monerris A;Gattuso H;Roca-Sanjuán D;Tuñón I;Marazzi M;Dumont E;Monari A
通讯作者:
Monari A
影响因子:
7.3
作者:
Bom, D;Curran, DP;Burke, TG
通讯作者:
Burke, TG
DOI:
10.1101/087969348.20.217
发表时间:
1990
期刊:
Cold Spring Harbor Monograph Archive
影响因子:
--
作者:
J. Champoux
通讯作者:
J. Champoux