Synthesis and Antitumor Activity of Novel Water Soluble Derivatives of Camptothecin as Specific Inhibitors of Topoisomerase I

1995 ◽  
Vol 38 (3) ◽  
pp. 395-401 ◽  
Author(s):  
Michael J. Luzzio ◽  
Jeffrey M. Besterman ◽  
David L. Emerson ◽  
Michael G. Evans ◽  
Karen Lackey ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Topoisomerase I ◽  
Water Soluble ◽  
Derivatives Of ◽  
Specific Inhibitors

Water Soluble Inhibitors of Topoisomerase I:  Quaternary Salt Derivatives of Camptothecin

1996 ◽  
Vol 39 (3) ◽  
pp. 713-719 ◽  
Author(s):  
Karen Lackey ◽  
Daniel D. Sternbach ◽  
Dallas K. Croom ◽  
David L. Emerson ◽  
Michael G. Evans ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Quaternary Salt ◽  
Water Soluble ◽  
Derivatives Of

scholarly journals Synthesis and Antitumor Activity of 20(S)-Camptothecin Derivatives: Carbamate-Linked, Water-Soluble Derivatives of 7-Ethyl-10-hydroxycamptothecin.

1991 ◽  
Vol 39 (6) ◽  
pp. 1446-1454 ◽  
Author(s):  
Seigo SAWADA ◽  
Satoru OKAJIMA ◽  
Ritsuo AIYAMA ◽  
Ken-ichiro NOKATA ◽  
Tomio FURUTA ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Derivatives Of

ChemInform Abstract: Synthesis of Water-Soluble (Aminoalkyl)camptothecin Analogues: Inhibition of Topoisomerase I and Antitumor Activity.

ChemInform ◽  
2010 ◽  
Vol 22 (22) ◽  
pp. no-no
Author(s):  
W. D. KINGSBURY ◽  
J. C. BOEHM ◽  
D. R. JAKAS ◽  
K. G. HOLDEN ◽  
S. M. HECH ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Topoisomerase I ◽  
Water Soluble ◽  
Camptothecin Analogues

Synthesis of water-soluble (aminoalkyl)camptothecin analogs: inhibition of topoisomerase I and antitumor activity

1991 ◽  
Vol 34 (1) ◽  
pp. 98-107 ◽  
Author(s):  
William D. Kingsbury ◽  
Jeffrey C. Boehm ◽  
Dalia R. Jakas ◽  
Kenneth G. Holden ◽  
Sidney M. Hecht ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Topoisomerase I ◽  
Water Soluble ◽  
Camptothecin Analogs

Synthesis and evaluation of some water-soluble prodrugs and derivatives of taxol with antitumor activity

1992 ◽  
Vol 35 (1) ◽  
pp. 145-151 ◽  
Author(s):  
Abraham E. Mathew ◽  
Magdalena R. Mejillano ◽  
Jyoti P. Nath ◽  
Richard H. Himes ◽  
Valentino J. Stella
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Derivatives Of

Potential anticonvulsants: Substituted N-benzylidene derivatives of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins

1983 ◽  
Vol 48 (4) ◽  
pp. 1173-1186 ◽  
Author(s):  
Václav Bártl ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Marie Bartošová ◽  
Miroslav Protiva
Keyword(s):  
Acute Toxicity ◽  
Water Soluble ◽  
Hypotensive Activity ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Soluble Salts ◽  
Sleeping Time ◽  
Central Depression ◽  
Derivatives Of ◽  
Electroshock Seizures

Reactions of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins XIVa-XIVd with benzaldehyde, 3,4-dimethoxybenzaldehyde, 4-dimethylaminobenzaldehyde, salicylaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, 2-(2-dimethylaminoethoxy)benzaldehyde, 3-(2-dimethylaminoethoxy)benzaldehyde and 3-ethoxy-4-(2-dimethylaminoethoxy)benzaldehyde afforded a series of 19 hydrazones IIIa-Xc. Some of them showed the expected anticonvulsant effect but only towards pentetrazole; antagonism of maximal electroshock seizures was not observed. In general, the products have a character of tranquillizers: in higher does they produce central depression, potentiate the thiopental sleeping time, have hypothermic action; in single cases antiamphetamine, antireserpine, antihistamine and cataleptic effects were observed. The water-soluble salts of the basic hydrazones VIIIa, VIIIc, IXc and Xc, administered parenterally, showed a rather high acute toxicity and revealed also adrenolytic and hypotensive activity.

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