Carboxyamidotriazole (L651582) is a carboxyamide-amino-imidazole compound originally developed as a coccidiostat, an antiprotozoal agent that acts upon Coccidia parasites. Carboxyamidotriazole (L651582) is an orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2 channels, blocking both Ca2 influx into cells and Ca2 release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion, and metastasis.

Rubitecan [Orathecin™] is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral compound being developed for the treatment of pancreatic cancer and other solid tumours by SuperGen. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.

Diphenyl acetamidotrichloroethyl fluoronitrophenyl thiourea, CGK733, was claimed to be selective inhibitor of the ataxia telangiectasia-mutated (ATM) protein and ATM- and Rad3-related (ATR) protein, however after investigation of the contents of the original paper by Korean Advanced Institute of Science and Technology (KAIST) several irregularities has been revealed and the paper was retracted in full. Further studies were completed showing that CGK-733 has no specific inhibitory effect on ATM or ATR. Unfortunately, the compound is still being marketed as an ATM/ATR inhibitor. CGK733 inhibits the proliferation of human cancer and non-transformed mouse fibroblast cell lines and induced senescent breast, lung, and colon carcinoma cells to undergo cell death.

Ginsenoside Rb3 is a protopanaxadiol ginsenoside that can be isolated from several different Panax species. Ginsenoside Rb3 exerts antidepressant and antidiabetic activities as well as cardio- and neroprotective action in ischemic tissue injury in animal models. Ginsenoside Rb3 inhibits apoptosis and cell proliferation, in addition it demonstrates antiaxidant properties. Ginsenoside Rb3 may modulate activity of GABA-A and NMDA receptors.

Norspermidine (1,7-diamino-4-azaheptane or dipropylenetriamine) is a structural homologue of the natural polyamine spermidine. Norspermidine and its metal complexes exert antineoplastic properties. Dipropylenetriamine NONOate is used as a donor of nitric oxide.