Angiogenesis reduction

An artemisinin-fullerene hybrid 92, Fig. 7) was described by Jung et al Hybrid 92, inhibited by 50% angiogenesis processes at 5 nmol/egg, was were found to be more potent than malonate-linked dimer of artemisinin by itself (only 14% of reduction was observed). ... 

Penicillamine (Cuprimine) can be used to treat acute, severe rheumatoid arthritis, producing reductions in joint pain, edema, and stiffness. The response to penicillamine is usually delayed (4-12 weeks), and remissions can last several months after withdrawal of treatment. Radiographic evidence of this drug s efficacy is limited thus, penicillamine is seldom used to treat rheumatoid arthritis. The mechanism of action of penicillamine is unknown, but some evidence suggests that it may involve the inhibition of angiogenesis, synovial fibroblast proliferation, or transcriptional activation. Because penicillamine can chelate copper and promote its excretion, it is used to treat Wilson s disease (hepatolenticular degeneration) and has also been used in mercury and lead intoxication. 

Angiogenesis inhibition. Cigarette smoke or smoke extract, administered to ulcerated rats once daily for 3 days, produced concomitant and dose-dependent reduction of angiogenesis and constitutive nitric oxide synthase activity . ... 

Borrelidin 1 has attracted attention because it inhibits angiogenesis, and so potentially blocks tumor growth, with an IC of 0.8 nM. Retrosynthetic analysis of 1 led the investigators to the prospective intermediates 2 and 3. To assemble these two fragments, they interatively deployed the elegant enantio- and diastereoselective intermolecular reductive ester aldol condensation that they had recently developed. This transformation is exemplified by the homologation of 4 to 6 catalyzed by the enantiomerically-pure Ir complex 5. 

---