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Research Article

Novel benzothiazolyl urea and thiourea derivatives with potential cytotoxic and antimicrobial activities

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Pages 57-64 | Received 09 Jul 2006, Accepted 10 Aug 2006, Published online: 04 Oct 2008

Figures & data

Figure 1 Some biologically active benzothiazoles: Antitumor agent (I) and HIV reverse transcriptase inhibitor (II).

Figure 1 Some biologically active benzothiazoles: Antitumor agent (I) and HIV reverse transcriptase inhibitor (II).

Figure 2 Potent telomerase inhibitors through G-quadruplex stabilization.

Figure 2 Potent telomerase inhibitors through G-quadruplex stabilization.

Scheme 1 The synthetic pathway of 2a, 2b.

Scheme 1 The synthetic pathway of 2a, 2b.

Scheme 2 The synthetic pathway of 3–6.

Scheme 2 The synthetic pathway of 3–6.

Table I.  Primary in vitro growth inhibition assay results for compounds at 100 and 10 μM concentration.

Figure 3 3D View from a molecular modeling study, of the minimum-energy structure of the complex of IV docked in the G-quadruplex of human telomere DNA (PDB ID: 1H1L). White dashed lines depict hydrogen bond interactions. Viewed using Molecular Operating Environment (MOE) module. (See colour online)

Figure 3 3D View from a molecular modeling study, of the minimum-energy structure of the complex of IV docked in the G-quadruplex of human telomere DNA (PDB ID: 1H1L). White dashed lines depict hydrogen bond interactions. Viewed using Molecular Operating Environment (MOE) module. (See colour online)

Figure 4 3D View from a molecular modeling study, of the minimum-energy structure of the complex of 3 docked in the G-quadruplex of human telomere DNA (PDB ID: 1H1L). White dashed lines depict hydrogen bond interactions. Viewed using Molecular Operating Environment (MOE) module. (See colour online)

Figure 4 3D View from a molecular modeling study, of the minimum-energy structure of the complex of 3 docked in the G-quadruplex of human telomere DNA (PDB ID: 1H1L). White dashed lines depict hydrogen bond interactions. Viewed using Molecular Operating Environment (MOE) module. (See colour online)

Table II.  Antimycobacterial in vitro activity of test compounds.

Table III.  Minimal inhibitory concentrations (MIC) in μg mL−1 of test compounds.

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