Portfolio of hits


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)


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)


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)


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


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


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)