New sulphonamide and carboxamide derivatives of acyclic C-nucleosides of triazolo-thiadiazole and the thiadiazine analogues. Synthesis, anti-HIV, and antitumor activities. Part 2.
A new series of acyclic C-nucleosides 1',2'-O-isopropylidene-D-ribo-tetritol-1-yl)[1,2,4] triazolo[3,4-b][1,3,4]thiadiazoles bearing arylsulfonamide (5-8) and arylcarboxamide (9-12) residues have been synthesized under microwave irradiation. Thiadiazines 13-15 have been analogously prepared, and upon acid hydrolysis, afforded the free nucleosides 16-18. The new synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound 7 was also screened against a panel of tumor cell lines consisting of CD4 human T-cells.
Al-Masoudi
Najim A
NA
Fachbereich Chemie, Universitat Konstanz, Konstanz, Germany. Najim.Al-Masoudi@gmx.de
Al-Soud
Yaseen A
YA
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D006839:Hydrocarbons, Acyclic / Q000737:chemistry*; D008872:Microwaves; D015394:Molecular Structure; D009705:Nucleosides / Q000737:chemistry*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013601:T-Lymphocytes / Q000187:drug effects; D013829:Thiadiazines / Q000737:chemistry*; D013830:Thiadiazoles / Q000737:chemistry*
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D006839:Hydrocarbons, Acyclic; D009705:Nucleosides; D013449:Sulfonamides; D013829:Thiadiazines; D013830:Thiadiazoles