RI-1 is a cell-permeable RAD51 inhibitor that binds covalently to the protein surface at Cysteine 319. RI-1 disrupts homologous recombination in human cells. Also, it is an inhibitor of Bfl-1 protein. RI-1 represents a powerful tool for future investigations on mechanisms of DNA repair. RI-1 holds promise as an oncologic drug. In a glioma xenograft model, the Rad51 inhibitor RI-1 clearly enhanced the effect of lomustine on tumor growth.

Grindelic acid is a labdane-type diterpene that was reported as the main secondary metabolite from Grindelia chiloensis Cabr and G. pulchella Dunal var. pulchella (Asteraceae). Recent studies demonstrated potential pharmaceutical applications for grindelic acid and its synthetic derivatives. Grindelic acid is a NOX4 inhibitor (IC50 2 uM). Grindelic acid’s mechanism of action is unknown, but it inhibited neither ROS in a cell-free membrane-based NOX4 assay nor from the purified NOX4 dehydrogenase domain. Grindelic acid demonstrates in vitro antitumor activity against human breast, cervix, lung,colon cancer.

Andrograpanin is a component of Andrographis paniculata, a traditional Chinese medicine (TCM) that has been effectively used for treatment of infection, inflammation, cold, fever, and diarrhea in China. Andrograpanin inhibited productions of NO and pro-inflammatory cytokines through down-regulating iNOS and pro-inflammatory cytokines gene expression levels. Further studies suggested that down-regulation of p38 mitogen-activated protein kinase (MAPKs) signaling pathways were involved in the anti-inflammatory activities of andrograpanin. This study provided evidences that andrograpanin might be useful as a potential anti-inflammatory leading compound for inflammatory drug development. Andrograpanin has the potential to modulate the chemokine pathway and the effect of andrograpanin might contribute to the anti-infectious function of A. paniculata.

BMS-794833 (N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-5-(4- fluorophenyl)-4-oxo-l,4-dihydropyridine-3-carboxamide) is an inhibitor of Met, VEGFR2, Ron, Axl and Flt-3 kinases. BMS-794833 demonstrated dose-dependent tumor growth inhibition following oral administration in xenograft models. In cell culture, BMS-794833 inhibited the proliferation of human tumor cell lines containing constitutively activated Met receptor. BMS-794833 is an active moety of pro-drug BMS-817378. Bristol-Myers Squibb and Simcere Pharmaceutical Group are developing BMS-817378 for treatment of cancer.