Antitumor and immunosuppressive activity of Merbarone's analogues and arylidenehydrazinopyrimidines.
The synthesis of Merbarone's analogues, the 4-thio- or 4-oxo derivatives of 5-carbamoyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine is described, starting from 5-carboxy-6-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidine+ ++. That was also used as staring material for synthesis of NCS624947 analogues, the 4-arylidenehydrazino-5-carbamoylpyrimidines. The reduction of arylidenehydrazinopyrimidines with hydrogen on Pd/C was also performed. The obtained compounds were successfully tested for anticancer and immunomodulating activity.
Długosz
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A
Department of Organic Chemistry, Faculty of Pharmacy, University of Medicine, Wrocław, Poland.
Machoń
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Z
D000818:Animals; D000917:Antibody Formation / Q000187:drug effects; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D007075:Immunoglobulin M / Q000096:biosynthesis; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012756:Sheep / Q000276:immunology; D013154:Spleen / Q000166:cytology / Q000187:drug effects / Q000276:immunology; D013858:Thiobarbiturates / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D006834:Hydrazines; D007075:Immunoglobulin M; D007166:Immunosuppressive Agents; D011743:Pyrimidines; D013858:Thiobarbiturates; C045459:merbarone