Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1232-5. doi: 10.1016/j.bmcl.2015.01.058.

Penta Ashok ¹, Subhash Chander ², Jan Balzarini ³, Christophe Pannecouque ³, Sankaranarayanan Murugesan ⁴

Affiliations

1 Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address: penta.ashok@gmail.com.
2 Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India.
3 Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
4 Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address: murugesan@pilani.bits-pilani.ac.in.

PMID: 25682562 DOI: 10.1016/j.bmcl.2015.01.058

Abstract

In the present study, a new series of β-carboline derivatives were synthesized and evaluated for inhibition activity against both HIV-1 and HIV-2 strains. Among these reported analogues, surprisingly (1-phenyl-9H-pyrido[3,4-b]indol-3-yl)(4-p-tolylpiperazin-1-yl)methanone (7b), (4-(2-methoxyphenyl)piperazin-1-yl)(1-phenyl-9H-pyrido[3,4-b]indol-3-yl)methanone (7f), (4-(4-fluorophenyl)piperazin-1-yl)(1-phenyl-9H-pyrido[3,4-b]indol-3-yl)methanone (7k), (4-(2-fluorophenyl)piperazin-1-yl)(1-phenyl-9H-pyrido[3,4-b]indol-3-yl)methanone (7l) displayed selective inhibition of HIV-2 strain with EC50 values of 3.3, 3.2, 2.6 and 5.4μM, respectively, which are comparable with nucleoside Reverse Transcriptase inhibitors lamivudine and dideoxyinosine. As these analogues have not shown in vitro HIV-2 Reverse Transcriptase inhibition, it could be excluded as potential target for their specific anti-HIV-2 activity.

Keywords

HIV-1; HIV-2; Reverse transcriptase; β-Carboline.

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