title: Synthesis, antitumor and antibacterial activities of some novel tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives.
abstract: Two series of new tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidines namely 2,3-disubstituted derivatives 3a-z and 2,4-disubstituted ones 6a-c were prepared and tested for their antitumor and antibacterial activities. The structures of the prepared compounds were confirmed by spectral and elemental analyses. Compound 3z exhibited the highest antitumor activity against breast MCF-7 with IC50 = 0.19 μM compared to Doxorubicin (IC50 = 5.46 μM), while 3r was the most active one against liver HEPG-2 cancer cell line with IC50 = 1.29 μM as regard to Doxorubicin (IC50 = 7.36 μM). Concerning the antibacterial activity, compounds 3m and 3z exerted remarkable activity against the tested bacterial species compared to Ampicillin, whereas compound 6c showed good activity against only Gram positive species.
authors.affiliation: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-Kasr El Aini Street, 11562 Cairo, Egypt.
authors.forename: Safinaz E
authors.initials: SE
authors.lastname: Abbas
authors.forename: Nagwa M
authors.initials: NM
authors.lastname: Abdel Gawad
authors.forename: Riham F
authors.initials: RF
authors.lastname: George
authors.forename: Yahya A
authors.initials: YA
authors.lastname: Akar
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents
keywords: Antibacterial activity; Antitumor activity; HEPG-2; MCF-7; Thieno[2,3-d]pyrimidines