title: Synthesis and anticancer evaluation of novel 2-cyclopropylimidazo[2,1-b][1,3,4]-thiadiazole derivatives.
abstract: A series of 2,5,6-trisubstituted imidazo[2,1-b][1,3,4]-thiadiazole derivatives 4(a-k) have been prepared by reaction of 2-amino-5-cyclopropyl-1,3,4-thiadiazole and an appropriate phenacyl bromide. Further 5-bromo 5(a-k) and 5-thiocyanato 6(a-k) derivatives were synthesized in order to study the effect of these substituents on antitumor activity. Structures of these compounds were established by IR, (1)H NMR, (13)C NMR and Mass spectroscopy. Seven compounds were granted NSC code at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10(-5) M) in full NCI 60 cell panel. Among the compounds tested, 5-bromo-6-(4-chlorophenyl)-2-cyclopropylimidazo[2,1-b][1,3,4]thiadiazole 5b (NSC D-96022/1) was found to be the most active candidate of the series at five dose level screening with degree of selectivity toward Leukemic cancer cell line.
authors.affiliation: Department of Pharmaceutical Chemistry, ASBASJSM College of Pharmacy, Bela, Ropar 140111, Punjab, India. mnoolvi@yahoo.co.uk
authors.forename: Malleshappa N
authors.initials: MN
authors.lastname: Noolvi
authors.forename: Harun M
authors.initials: HM
authors.lastname: Patel
authors.forename: Navjot
authors.initials: N
authors.lastname: Singh
authors.forename: Andanappa K
authors.initials: AK
authors.lastname: Gadad
authors.forename: Swaranjit Singh
authors.initials: SS
authors.lastname: Cameotra
authors.forename: Arvind
authors.initials: A
authors.lastname: Badiger
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013055:Spectrophotometry, Infrared; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole