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Subhas Karki, Rahul Hazare, Sujeet Kumar, Vivek Bhadauria, Jan Balzarini and Erik De Clercq

Synthesis, anticancer and cytostatic activity of some 6H-indolo[2,3-b]quinoxalines

Various 6-aralkyl-9-substituted-6H-indolo[2,3-b]quinoxalines were synthesized by reaction of 1,5-disubstituted 2,3-dioxo-2,3-dihydroindole with orthophenylene diamine. Appreciable anticancer activity of compounds 5b, 5d, 5g and 5l at various cell lines among 59 human tumor cell panels was observed. All the synthesized compounds were evaluated for cytostatic activity against human Molt 4/C8 and CEM T-lymphocytes as well as for murine L1210 leukemia cells. Compound 5h exhibited an IC 50 of 71 µmol mL-1 against Molt 4/C8 and 117 µmol mL-1 against CEM compared to melphalan 3.2 µmol mL-1 and 2.5 µmol mL-1, respectively. The IC 50 for compound 7i against L1210 was 7.2 µmol mL-1 compared to melphalan 2.1 µmol mL-1.

Open access

Yaseen Al-Soud, Najim Al-Masoudi, Hamed Hassan, Erik De Clercq and Christophe Pannecouque

Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives

A series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H- -imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and alkyl- [4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin- -1-yl)ketones (11-20) as well as the indole analogue 22 were synthesized from 4-nitro-5-piperazinyl imidazole derivative 1, with the aim to develop newly non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound 2 showed inhibition of HIV-1 (EC50 0.45 mg mL-1) and HIV-2 (0.50 mg mL-1), while 9 showed inhibition of HIV-1 (EC50 2.48 mg mL-1, SI = 4).