OpenSourceMalaria / Series3

Everything to do with Open Source Malaria Series 3
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Compounds for biological testing Nov 2018 (including SGS-UNC compounds) #11

Closed mbhebhe closed 5 years ago

mbhebhe commented 5 years ago

Compounds for biological testing. # USyd samples to be sent end of next week. OSM-S-606 is a product of the bromination of pyrrole occurring at the 7th position. OSM-S-137 (slightly active at 1.7 uM) was re-synthesized for sending to Kansas State Uni and UNC for kinome testing. OSM-S-145 was synthesised but not tested and came across it in the fridge.

SGS-UNC samples to be sent soon. These samples were made by Alfredo Picado from SGS-University of North Carolina. They are similar to our Series 3 compounds. We will see if they have any activity. #8

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These compounds will be sent with the S4 compounds. Once we have the biological data, it can be found on here

November 2018 Dundee.zip

MFernflower commented 5 years ago

@mbhebhe do you have the required boronic acid to make the carboxylic acid analogue of the original hit?

mbhebhe commented 5 years ago

Not yet. I will try and make it and hopefully in time for the shipment

MFernflower commented 5 years ago

considering how close our lead is to caboxamycin - do you think it'd be worth coupling the thieno core to some two and three hydroxyphenyl boronic acid? @mbhebhe @holeung

MFernflower commented 5 years ago

Closing this issue - see https://github.com/OpenSourceMalaria/Series4/issues/62 for potency results once they come in!