Control compounds : MMV897698 as the reference compound (#572); MMV663915 resynthesis by SSP students of this year; additional test for OHOH pfizer compound #36.
SSP compounds: set of compounds made by SSP program students at Sydney University earlier this year, in some cases tele-substituted products were isolated as well.
Miscellaneous compounds: most of these compounds were made as a part of investigation of tele-substitution reaction.
So as competition is over - here are results for the august batch:
Control and retest:
Control OSM-S-369 showed result 362 nM comparable to previous 251nM, 301nM, 534 nM;
OSM-S-293 remade by SSP students confirmed high potency 136 nM (previous 166 nM);
OHOH compound OSM-S-556 was retested again but once again we were unable to replicate potency of original biosynthesis 605 nM (previous 659 nM, 146 nM).
General observations:
Tele-substitution products are generally inactive, what is in alignment with previous results;
Sterically bulky substituents (eg. antracenyl or tertbutylphenyl) on triazole ring are not tolerated;
Electron rich aromatic substituents on triazole ring are not tolerated;
OSM-S-651 (0.367 uM) has surprisingly higher potency than unprotected analogue OSM-S-609 (6.132 uM), presumably due to lower polarity and thus improved cell penetration
Results are at bottom of thread!
2019.08.16 - Dundee Shipment.zip