4-Aroyl-1-nitrosohydrazinecarboxamides: synthesis, in vivo and in vitro antitumor activity

 
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4-Aroyl-1-nitrosohydrazinecarboxamides: synthesis, in vivo and in vitro antitumor activity

Mourelatos, Dionysios
Topakbashian, VV.
Boutis, Lazaros
Golovisky, Ev.
Dozi-Vassiliades, J.
Taksirov, SI.
Papageorgiou, Athanasios
Margariti, E.
Gugova, RG.

4-Benzoyl-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide (I), 1-(2-chloroethyl)-1-nitroso-4-phenylacetylhydrazine-carboxamide (II), 1-(2-chloroethyl)-4-(2-hydroxybenzoyl)-1-nitrosohydrazinecarboxamide (III), 4-(4-aminobenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide (IV), 4-(4-chlorobenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide (V), all novel class nitrosoureas, were synthesized. All five compounds showed a dose-dependent activity against leukemias L1210, P388 and Ehrlich ascites tumor (EAT). Compound I was superior, yielding T/C% values of 400%, resulting in many cures, reaching 100% in EAT mice. The effect of the above substances on the incorporation of radioactive precursors into DNA, RNA and proteins of EAT cells was investigated. It was found that treatment of cells with 50 mug/ml of the compounds causes significant inhibition (approximately 70%) of the incorporation of H-3-thymidine into DNA. Finally, the effect of these compounds on sister chromatid exchange (SCE) values and on cell kinetics in cultured human lymphocytes was studied. Compound I was found to be the most effective in causing markedly increased SCE values and cell division delays.

Article / Άρθρο
info:eu-repo/semantics/article

Αριστοτέλειο Πανεπιστήμιο Θεσσαλονίκης (EL)
Aristotle University of Thessaloniki (EN)

Αγγλική γλώσσα

1992
2009-07-17T10:15:32Z


Αριστοτέλειο Πανεπιστήμιο Θεσσαλονίκης, Σχολή Επιστημών Υγείας, Τμήμα Ιατρικής

urn:ISSN:02235234
European Journal of Medicinal Chemistry, vol.27 , no. 8 [1992] p.745-750 [Published Version]

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