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20th February 2013 @ 02:46

Biological evaluation of OSM-S-106 through 116 (excluding OSM-S-107) performed in Vicky Avery's lab by Sabine Fletcher.

The compounds look good in this round - all but cpd OSM-S-113 show activity.

I already ran the cytotoxicity as well, and none of the compounds was particularly cytotoxic (see 'summary report' file and curves in PDF).

Solubility: minor floating specks after dissolving in OSM-S-106; all others fine

Unfortunately I made a minor mistake: I started the Artemisinin CRC curve at the wrong concentration, 40 uM (same concentration as the compounds) as opposed to the usual 2 uM. The IC50 value obtained for the control is correct (4 nM), just the x-axis range of the curve is different compared to the previous runs. Sorry for that!



Displacement Curves

2013_02_19 Sydney cpds batch 4 on 3D7 page1.pdf
2013_02_19 Sydney cpds batch 4 on 3D7 page 2.pdf

2013_02_19 Sydney cpds batch 4 on HEK page 1.pdf


ID InChI 3D7 IC50 (nM)
OSM-S-106  InChI=1S/C12H10N4O2S2/c13-12-11-9(15-6-16-12)5-10(19-11)7-2-1-3-8(4-7)20(14,17)18/h1-6H,(H2,13,15,16)(H2,14,17,18)  36
OSM-S-108  InChI=1S/C16H15N3OS/c1-10-8-12(11(2)17-10)9-14-15(20)19-16(21-14)18-13-6-4-3-5-7-13/h3-9,17H,1-2H3,(H,18,19,20)/b14-9-  1200
 OSM-S-109  InChI=1S/C22H18N4O3S/c1-14-12-16(15(2)25(14)18-8-10-19(11-9-18)26(28)29)13-20-21(27)24-22(30-20)23-17-6-4-3-5-7-17/h3-13H,1-2H3,(H,23,24,27)/b20-13-  262
 OSM-S-110  InChI=1S/C22H18N4O4S/c1-13-10-15(14(2)25(13)17-6-8-18(9-7-17)26(29)30)11-20-21(28)24-22(31-20)23-16-4-3-5-19(27)12-16/h3-12,27H,1-2H3,(H,23,24,28)/b20-11-  2300
 OSM-S-111   InChI=1S/C23H21N3O2S/c1-15-13-17(16(2)26(15)19-9-11-20(28-3)12-10-19)14-21-22(27)25-23(29-21)24-18-7-5-4-6-8-18/h4-14H,1-3H3,(H,24,25,27)/b21-14-  146


 OSM-S-113  InChI=1S/C21H18N4O2S/c1-13-11-15(14(2)25(13)19-5-3-4-10-22-19)12-18-20(27)24-21(28-18)23-16-6-8-17(26)9-7-16/h3-12,26H,1-2H3,(H,23,24,27)/b18-12-  >40,000




OSM-S-35  InChI=1S/C22H19N3OS/c1-15-13-17(16(2)25(15)19-11-7-4-8-12-19)14-20-21(26)24-22(27-20)23-18-9-5-3-6-10-18/h3-14H,1-2H3,(H,23,24,26)/b20-14-  38
OSM-S-116 InChI=1S/C16H17FN2O3/c1-9-8-14(16(21)22-11(3)15(18)20)10(2)19(9)13-6-4-12(17)5-7-13/h4-8,11H,1-3H3,(H2,18,20)  11000


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19th February 2013 @ 06:41

Glutathione Trapping Study for OSM-S-35 



CDCO_MMV_OSDD_13_001_Met ID.xlsx
CDCO_MMV_OSDD_13_001_Met ID.pdf


We’ve run the glutathione trapping study for OSM-S-35 in the presence of metabolic activation (i.e. human microsomes). We also included a search for other potential metabolites formed. A number of metabolites were detected, mainly oxygenated species (mono, bis and tri-oxygenated metabolites) with the predominant metabolite (based on peak area and assuming similar response factors for each metabolite) arising from likely hydroxylation of the pyrrole substituted benzene. In the presence of GSH-EE, adducts were observed both in the presence and absence of metabolic activation. The results are summarised in the attached file. Please let me or Sue know if you have any questions or comments

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