Syntheses of optically active monapterin, 7,8-dihydromonapterin, and 5,6,7,8-tetrahydromonapterin from l-xylose.

We describe the syntheses of monapterin, dihydromonapterin and tetrahydromonapterin in optically active forms. The syntheses involved the condensation of l-xylose with phenylhydrazine, providing a hydrazone derivative. The reaction of the resulting hydrazone with triamino-pyrimidinone followed by oxidation of the resulting pteridinone with molecular oxygen furnished pterin containing a hydroxylated side chain.

Functionalized azirine based scaffolds as endothelin inhibitors for the selective anti-angiogenic activity.

Anti-angiogenic therapy has long been used as an adjunct therapy for the resolution of tumor burden. The current findings describe the synthesis of novel marine-based azirine-containing compounds that exhibit anti-angiogenic mediated anti-tumor activity. Azirine-2-carboxylate inhibited HUVEC-mediated tubulogenesis without causing cell death in a dose-dependent manner.