Synthesis and antiproliferative activity of conjugates of adenosine with muramyl dipeptide and nor-muramyl dipeptide derivatives.

We synthesized a series of MDP(D,D) and nor-MDP(D,D) derivatives conjugated with adenosine through a spacer as potential immunosuppressants. New conjugates 8a-k were evaluated on two leukemia cell lines (Jurkat and L1210) and PBMC from healthy donors. The conjugates 8a-k and MDP(D,D)/nor-MDP(D,D) derivatives 7e, f, i, j were active against L1210 cell line.

[Adenosine, its analogues and conjugates].

Adenosine is an endogenous purine nucleoside that plays an important role in many biochemical processes. It acts through the four types of adenosine receptors: A1, A2A, A2B, A3 which are located i.a.

Therapeutic potential of adenosine analogues and conjugates.

This review summarizes current knowledge of adenosine analogues and conjugates with promising therapeutic properties. Adenosine is a signaling molecule that triggers numerous physiological responses. It acts through the adenosine receptors (ARs), belonging to the family of G-protein-coupled receptors and widely distributed throughout the body.

Synthesis of novel aryl(heteroaryl)sulfonyl ureas of possible biological interest.

The course of reaction of aryl and heteroaryl sulfonamides with diphenylcarbonate (DPC) and 4-dimethylaminopyridine (DMAP) was found to depend on the pKa of the sulfonamide used. Aryl sulfonamides with pKa approximately 10 gave 4-dimethylamino-pyridinium arylsulfonyl-carbamoylides, while the more acidic heteroaryl sulfonamides (pKa approximately 8) furnished 4-dimethylaminopyridinium heteroarylsulfonyl carbamates. Both the carbamoylides and carbamate salts reacted with aliphatic and aromatic amines with the formation of appropriate aryl(heteroaryl)sulfonyl ureas, and therefore, can be regarded as safe and stable substitutes of the hazardous and difficult to handle aryl(heteroaryl)sulfonyl isocyanates.