Scott, FJ;
Nichol, RJO;
Khalaf, AI;
Giordani, F;
Gillingwater, K;
Ramu, S;
Elliott, A;
... Suckling, CJ; + view all
(2017)
An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics.
European Journal of Medicinal Chemistry
, 136
pp. 561-572.
10.1016/j.ejmech.2017.05.039.
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Abstract
This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC₈₀s of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MIC₉₉s of 3.1 μM against the mycobacterium M. tuberculosis. The selectivity and activity of these compounds is related to their physicochemical properties and the cell wall/membrane characteristics of the infective agents.
| Type: | Article |
|---|---|
| Title: | An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.ejmech.2017.05.039 |
| Publisher version: | https://doi.org/10.1016/j.ejmech.2017.05.039 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| Keywords: | Minor Groove Binders, Anti-infective, Antifungal, Anti-tuberculosis |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > UCL BEAMS UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Physics and Astronomy |
| URI: | https://discovery-pp.ucl.ac.uk/id/eprint/10073748 |
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