title: Synthesis, in vitro antimicrobial and in vivo antitumor evaluation of novel pyrimidoquinolines and its nucleoside derivatives.
abstract: Seven series of pyrimidoquinoline derivatives have been synthesized, tetrazolo[4',3':-1,2]pyrimido[4,5-b]quinoline (3), 2-aminopyrimido[4,5-b]quinoline (4), triazolo[4',3':1,2]-pyrimidoquinoline (5a,b, 10), imidazolo[3',2':1,2]pyrimido[4,5-b]-quinoline (8a,b), 6-chloro-2-methylthiopyrimido[4,5-b]quinoline (12), acetylated nucleosides (16, 17a,b) and deacetylated nucleosides (18, 19a,b). Some of the novel pyrimidoquinoline derivatives possess highly activity toward the bacteria and fungi species. The new quinolines derivatives were evaluated for their anticancer activity toward human cancer cell lines by the National Cancer Institute (NCI). Most of them had excellent growth inhibition activity, having LD(50) values in the low micromolar to nanomolar concentration range.
authors.affiliation: Photochemistry Department, National Research Centre, 12622 Dokki, Cairo, Egypt. hebanrc@yahoo.com
authors.forename: Hebat-Allah S
authors.initials: HA
authors.lastname: Abbas
authors.forename: Hend N
authors.initials: HN
authors.lastname: Hafez
authors.forename: Abdel-Rahman B A
authors.initials: AR
authors.lastname: El-Gazzar
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001419:Bacteria / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D005658:Fungi / Q000187:drug effects; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D009705:Nucleosides / Q000737:chemistry*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D009705:Nucleosides; D011804:Quinolines