title: SYNTHESIS, ANTI-HEPATITIS B AND C VIRUS ACTIVITY AND ANTITUMOR SCREENING OF NOVEL THIAZOLO[4,5-D]-PYRIMIDINE DERIVATIVES.
abstract: The paper describes the synthesis, antivirus and antitumor evaluation of novel thiazolo[4,5-d]pyrim- idine derivatives. The target compounds 3a-h were synthesized by cyclocondensation of 4-amino-N'-(phenyl- methylidene)-3-phenyl-2-thioxo-2,3-dihydrothiazole-5-carbohydrazides 2a-d with aromatic aldehydes. The structures of new compounds were determined by IR, ¹H-NMR and elemental analysis. Thiazolopyrimidines 3a and 3d-h were screened by the National Institute of Allergy and Infectious Diseases against various viruses. Four compounds 3e-h showed in vitro anti-HCV activity. One (3e) demonstrated significant activity against HBV and was submitted to an anti-HBV in vivo assay but had a low bioavailability. As a result of antitumor study, compound 3h was found to be most potent against leukemia SR.
authors.forename: Lilianna
authors.initials: L
authors.lastname: Becan
authors.forename: Anna
authors.initials: A
authors.lastname: Wójcicka
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D016174:Hepacivirus / Q000187:drug effects*; D006515:Hepatitis B virus / Q000187:drug effects*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D000998:Antiviral Agents; D011743:Pyrimidines; D013844:Thiazoles