Synthesis and antitumor activity of substituted triazolo[4,3-a]pyrimidin-6-sulfonamide with an incorporated thiazolidinone moiety.
Chlorosulfonation of 3-methyl[1,2,4]triazolo[4,3-a]pyrimidine with chlorosulfonic acid in the presence of thionyl chloride was studied. When triazolo[4,3-a]pyrimidines are used as substrates, the substitution occurs at C-6. Also the reactivity of the hydrazides (7) towards aldehydes, thioglycolic acid and amines were studies. The newly prepared compounds 10a,d and 11a,d demonstrated inhibitory effects on the growth of a wide range of cancer cell lines generally at 10(-5)M level and in some cases at 10(-7)M concentrations.
Hafez
Hend N
HN
National Research Centre, Photochemistry Department (Heterocyclic & Nucleoside Unit), Dokki, 12622 Cairo, Egypt. hendnagah2000@yahoo.com
El-Gazzar
Abdel-Rahman B A
AR
D000577:Amides / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D002470:Cell Survival; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008956:Models, Chemical; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D013461:Sulfur Oxides / Q000737:chemistry; D013844:Thiazoles / Q000737:chemistry*
D000577:Amides; D000970:Antineoplastic Agents; D011743:Pyrimidines; D013449:Sulfonamides; D013461:Sulfur Oxides; D013844:Thiazoles; C023589:thionyl chloride