Abstract
Synthesis and biological properties of 27 derivatives of 5-amino-3-methylisothiazolo[5,4-d]pyrimidine-4-dione and of 3-methyl-5-semicarbazido-4-isothiazolocarboxylic acid ethyl esters are discussed. 5-Amino-3-methylisothiazolo[5,4-d]pyrimidine-4-dione was converted by reaction with aldehydes into Schiff bases, which under reduction of NaBH4, were transformed into appropriate N-methylene analogs. 3-Methyl-5-semicarbazido-4-isothiazolocarboxylic acid ethyl esters in reaction with aldehydes were converted into benzylidene derivatives. Some of the compounds obtained, especially those of Schiff base structure, displayed strong activity against L-1210 leukemia, Sa-180 sarcoma. Ehrlich carcinoma and Nemeth Kellner lymphoma.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / therapeutic use*
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Carcinoma, Ehrlich Tumor / drug therapy
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Carcinoma, Ehrlich Tumor / pathology
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Cell Division / drug effects
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Chemical Phenomena
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Chemistry
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Drug Screening Assays, Antitumor
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Leukemia L1210 / drug therapy
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Leukemia L1210 / pathology
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Lymphoma / drug therapy
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Lymphoma / pathology
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Mice
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Mice, Inbred BALB C
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Mice, Inbred DBA
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Neoplasms, Experimental / drug therapy*
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Neoplasms, Experimental / pathology
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Pyrimidines / chemical synthesis
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Pyrimidines / therapeutic use*
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Sarcoma, Experimental / drug therapy
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Sarcoma, Experimental / pathology
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Thiazoles / chemical synthesis
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Thiazoles / therapeutic use*
Substances
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Antineoplastic Agents
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Pyrimidines
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Thiazoles