title: Synthesis and antitumor activity of new sulfonamide derivatives of thiadiazolo[3,2-a]pyrimidines.
abstract: New series of sulfonamide derivatives of [1,3,4]thiadiazolo[3,2-a]pyrimidine were synthesized and investigated as antitumor agents. Some of the newly prepared compounds were tested for their in vitro and in vivo antitumor activities. Preliminary biological studies revealed that compounds 4c, 4f, and 4j exhibited the highest affinity to DNA, while compounds 4h,i, 6a-c, 8 and 12-14 exhibited moderate activity. Also, compounds 4j, 4f and 4c showed the highest percentage increase in lifespan of mice inoculated with Ehrlich ascites cells over 5-flurouracil (positive control). The detailed synthesis, spectroscopic and biological data are reported.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.
authors.forename: Nadia S
authors.initials: NS
authors.lastname: El-Sayed
authors.forename: Eman R
authors.initials: ER
authors.lastname: El-Bendary
authors.forename: Saadia M
authors.initials: SM
authors.lastname: El-Ashry
authors.forename: Mohammed M
authors.initials: MM
authors.lastname: El-Kerdawy
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002286:Carcinoma, Ehrlich Tumor / Q000473:pathology; D004247:DNA / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013449:Sulfonamides / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D011743:Pyrimidines; D013449:Sulfonamides; D004247:DNA