With the aim of fuelling open-source, translational, early-stage drug discovery activities, the results of the recently completed antimycobacterial phenotypic screening campaign against Mycobacterium bovis BCG with hit confirmation in M. tuberculosis H37Rv were made publicly accessible. A set of 177 potent non-cytotoxic H37Rv hits was identified and will be made available to maximize the potential impact of the compounds toward a chemical genetics/proteomics exercise, while at the same time providing a plethora of potential starting points for new synthetic lead-generation activities. Two additional drug-discovery-relevant datasets are included: a) a drug-like property analysis reflecting the latest lead-like guidelines and b) an early lead-generation package of the most promising hits within the clusters identified.

Reductive cyclization of nitrobiphenyls and nitrostyrenes to carbazoles and indoles, respectively, is carried out by triphenylphosphine under mild conditions catalyzed by a dichlorodioxomolybdenum(VI) complex. A one-pot procedure for the synthesis of regioselectively functionalized indoles has been developed from commercially available onitrobenzaldehydes and phosphoranes.

Chemoselective deoxygenation of sulfoxides to sulfides was carried out by P(OPh) 3 in mild conditions catalyzed by dichlorodioxomolybdenum(VI).

At room temperature, reacting cis-[Au(Ar)(M)Cl] with [PhCH2PPh3]Cl (l:l), with PPh3 plus NaC104*Hz0 (1:2:1), or with PPh3 (1:l) leads to a reductive elimination giving gold (1) complexes [PhCH2PPh3] [AuC12], [ A u ( P P~~)~] C~O , , or [AuCl(PPh3)], respectively, and in high yields, the corresponding biaryls Ar-Ar' [Ar = C6H4N=NPh-2, Ar' = Ar (l), C6H4NO2-2 (2), C6F6 (3); Ar = Ar' = C6H3(N=NC6H4Me-4')-2, Me-5 (4); Ar = C6H4CH2NMez-2, Ar' = P h (E), C6H4N=NPh-2 (61, C6H3(N=NC6H4Me-4')-2, Me-5 (711.

Chemoselective deoxygenation of N-oxides was carried out under mild conditions with common phosphines in the presence of dichlorodioxomolybdenum(VI).