Portfolio of hits

deoxy.tif

This N-(3’-deoxythymidin-3’-yl)-1-substituted-1H-tetrazol-5-arylamine with a 5-(2-bromovinyl) substituent is the most potent and selective mithondrial thymidine kinase (TK-2) inhibitor reported so far (IC50 = 14 nM; Org. Biomol. Chem. 2011, 9, 892-901)

galcer.tif

NU-α-GalCer, a Th1 biasing NKT cell agonist that occupies an extra binding pocket in mCD1d through induced fit (J. Am. Chem. Soc. 2008, 130, 16468-16469; EMBO J. 2011, 30, 2294-2305)

thymidine.tif

This α-thymidine derivative, featuring a 5’-(3-trifluoromethyl-4-chlorophenyl)-
thiourea moiety, was the first M. tuberculosis TMPK inhibitor (Ki of 0.6 µM) showing good inhibitory activity on growing M. bovis and M. tuberculosis, thereby promoting mycobacterial TMPK as an attractive target for inhibitor design (J. Med. Chem. 2007, 50, 5281-5292)

amino.tif

2’-Amino-2’-deoxy-2-thioUTP, most potent and selective P2Y2 agonist reported so far (J. Med. Chem. 2007, 50, 1166-1176)

dichlorophenyl.tif

α-Dichlorophenyl analogue of fosmidomycin that exhibits significantly improved in vitro antimalarial activity than fosmidomycin (Bioorg. Med. Chem. Lett. 2006, 16, 1888-1891)

adenosine.jpg

Hypermodified adenosine analogue with potent (Ki = 1.8 nM) fully agonistic A3AR activity and high A3/A1 selectivity (J. Med. Chem. 2006, 49, 7373-7383)