New analogues sent for biological testing JAN 2024

[yinuowang0812]

The following compounds were synthesised and sent to TGSLS for potency evaluation against P. falciparum 3D7. The results have been received as below.

• 106 positive control has a greater IC50 then previously testing. Asked TCGLS for retesting and will update here when I get the reply.
• New pyridyl sulfonamide OSM-LO-90 is inactive. Docking request will be sent.
• Benzyl sulfonamide OSM-LO-89 is moderately active.
• 106-Pro adduct (OSM-LO-91)is very active and I've asked TCGLS to do toxicity testing. This molecule is unlikely to be a selective cmpd as the Human Pro-RS is also expected to be a target from biological team's aspect but definitely adds to the rationale for the Yinuo Box.

TCGLS biological testing Jan 24.cdxml.zip TCGLS results 160224.pdf TCGLS results Jan 24.pdf

[yinuowang0812]

The results of the retesting of OSM-S-106 in this batch have been released. The IC50 is still significantly higher than previously observed, suggesting potential contamination during transferring or due to the containers. I am arranging a shipment of a fresh sample of OSM-S-106 to TCGLS.

The IC50 of the 106-Pro adduct (OSM-LO-91) remains impressive, and the toxicity data look very promising. I am in contact with TCGLS to ask about the exact value and reach out to Leann's team for suggestions on the biological aspects.

106: 106-Pro results .10324 TCGLS.pdf

[yinuowang0812]

OSM-LO-91 (YNW69, OSM-S-106-Pro-adduct) has been retested after removing the HCl salt. The potency remained.

TCGLS biological testing May 24.cdxml.zip

TCGLS results May 2024.pdf