ChemInform Abstract: SUBSTANCES WITH ANTINEOPLASTIC ACTIVITY. PART LXX. SOME 2-SUBSTITUTED DERIVATIVES OF 5-(2-AMINO-6-HYDROXY-4-OXO-3,4-DIHYDRO-5-PYRIMIDINYL)PENTANOIC ACID

1981 ◽  
Vol 12 (39) ◽  
Author(s):  
R. KOTVA ◽  
J. KREPELKA ◽  
A. CERNY ◽  
V. PUJMAN ◽  
M. SEMONSKY
Keyword(s):  
Antineoplastic Activity ◽  
Pentanoic Acid ◽  
Derivatives Of

Some 2-substitution derivatives of 5-(4-oxo-6-hydroxy-3,4-dihydro-5-pyrimidinyl)pentanoic acid

1983 ◽  
Vol 48 (1) ◽  
pp. 304-311 ◽  
Author(s):  
Jiří Křepelka ◽  
Jan Beneš ◽  
Vladimír Pouzar ◽  
Jaroslav Vachek ◽  
Jiří Holubek
Keyword(s):  
Nitrile Group ◽  
Antineoplastic Activity ◽  
Carboxyl Group ◽  
Positional Isomers ◽  
Pentanoic Acid ◽  
Pharmacological Tests ◽  
Derivatives Of

Condensation of triethyl ester of 1,1,5-pentanetricarboxylic acid (XI) with substituted guanidines XXII - XXIX gave acids II - IX, which were converted into esters XI - XIX. The acid II and the ester XI were obtained as mixtures of positional isomers. Analogously, condensation of the triester XXI with dicyanodiamide gave rise to acid X, whose nitrile group, under conditions of esterification of a carboxyl group, produced iminoether XX. In pharmacological tests for antineoplastic activity the compounds prepared exhibited weaker efficacy than 5-(2-amino-6-hydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acid (I), employed as standard.

Some 2-substituted derivatives of 5-(2-amino-6-hydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acid

1981 ◽  
Vol 46 (6) ◽  
pp. 1397-1404 ◽  
Author(s):  
Rudolf Kotva ◽  
Jiří Křepelka ◽  
Antonín Černý ◽  
Vojtěch Pujman ◽  
Miroslav Semonský
Keyword(s):  
Point Of View ◽  
Pentanoic Acid ◽  
Antineoplastic Effect ◽  
Derivatives Of

On condensation of 6-substituted trialkyl esters of 2-carboxy-1,7-heptanedioic acids XIII-XXIII with guanidineand subsequent saponification 2-substituted 5-(2-amino-6-hydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acids II-XII were prepared. From the pharmacological point of view some of the substances prepared had a potentiating effect on the antileukemia effect of 5-fluorouracil in mice and the antineoplastic effect manifested by a diminution of the tumours in animals with experimental tumours.

2-Substituted derivatives of 5-(4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acid

1982 ◽  
Vol 47 (9) ◽  
pp. 2525-2529 ◽  
Author(s):  
Rudolf Kotva ◽  
Jiří Křepelka ◽  
Jaroslav Vachek
Keyword(s):  
Pentanoic Acid ◽  
Antineoplastic Effect ◽  
Derivatives Of

Condensation of trialkyl esters of 6-substituted 2-carboxy-1,7-heptanedioic acids XII-XVII with urea or thiourea and subsequent saponification gave 2-substituted 5-(2,6-dihydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acids II-VI or 5-(2-mercapto-6-hydroxy-4-oxo-3,4-dihydro-6-pyrimidinyl)pentanoic acids VII-XI, respectively. Compounds II, VII and X had a weak antineoplastic effect in animals with experimental transplantable tumours.

Synthesis and Antineoplastic Activity of O-Alkylated Derivatives of 7-Hydroximinoandrost-5-ene Steroids

2010 ◽  
Vol 343 (7) ◽  
pp. 377-383 ◽  
Author(s):  
Ranju Bansal ◽  
Sheetal Guleria ◽  
Christina Ries ◽  
Rolf W. Hartmann
Keyword(s):  
Antineoplastic Activity ◽  
Derivatives Of
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