CCT-018159 is a novel inhibitor of heat shock protein (Hsp) 90 with potential anticancer activity. CCT-018159 inhibited human HSP90beta with comparable potency to 17-AAG and with similar ATP-competitive kinetics. The mean cellular GI(50) value of CCT-018159 across a panel of human cancer cell lines, including melanoma, was 5.3 mumol/L. CCT-018159 caused cell cytostasis associated with a G(1) arrest and induced apoptosis. CCT-018159 also inhibited key endothelial and tumor cell functions implicated in invasion and angiogenesis. CCT-018159 has the potential to inhibit invasion and angiogenesis as part of combinatorial anticancer effects. CCT-018159 is still in the preclinical development stage for the treatment of cancer.

Gomisin N is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. In vitro assays demonstrated that Gomisin N could inhibit TGF-β induced epithelial-mesenchymal transition of 4T1 cells and of primary human breast cancer cells. Gomisin N could maintain membrane stability of rat hepatocytes under oxidative stress. Gomisin N can reduce inflammation, inhibit apoptosis, and improve cardiac function after ischemic injury. It represents a potential novel therapeutic approach for treatment of ischemic heart disease. Gomisin N produced beneficial sedative and hypnotic bioactivity, which might be mediated by the modification of the serotonergic and GABAergic system.

Antimycin A is widely used as a piscicide in the catfish farming industry (brandname Fintrol) and has potent killing activity against insects, nematodes and fungi. Antimycin A is a potent inhibitor of ubiquinol-cytochrome C oxidoreductase (complex III). By inhibiting cytochrome C reductase in the electron transport chain of mitochondria antimycin A halts respiration. It has been used to study the metabolic signature of RCD in human cultured skeletal muscle cells. The specific sites of reactive oxygen species (ROS) production in mitochondria isolated from skeletal muscle of chronic obstructive pulmonary disease and lung cancer patients, and its relationship with local oxidative stress induced by exercise have been studied using antimycin A as well. More recently, antimycin A has attracted attention as a potent and selective inhibitor of the mitochondrial anti-apoptotic proteins Bcl-2 and Bcl-xL which are over-produced in cancer cells resistant to apoptosis-inducing chemotherapy agents, so antimycin A may have a potential as anticancer drug for combination chemotherapy.

Epothilone A is a natural compound, originally discovered from the myxobacterium Sorangium cellulosum. Epothilones A, a macrolide compound, stabilizes polymerized microtubules, leading to mitotic arrest and cytotoxicity in proliferating cells. While epothilone A shows potent antineoplastic activity in vitro, these effects were not seen in preclinical in vivo models due to its poor metabolic stability and unfavorable pharmacokinetics.

Meliltoside is a 2-glucosyloxycinnamic acid found in Dendrobium medicinal plants, Ajuga laxmannii, Ajuga chamaecistus ssp. tomentella, and Teloxys graveolens. It demonstrated moderate antiprotozoal and anti-cancer activity in vitro.

Monastrol is a small, cell-permeable molecule that arrests cells in mitosis by specifically inhibiting Eg5, a member of the Kinesin-5 family. Monastrol has been used to probe the dynamic organization of the mitotic spindle. Monastrol inhibits both the basal and the microtubule-stimulated ATPase activity of the Eg5 motor domain. Unlike many ATPase inhibitors, monastrol does not compete with ATP binding to Eg5. Monastrol appears to inhibit microtubule-stimulated ADP release from Eg5 but does not compete with microtubule binding, suggesting that monastrol binds a novel allosteric site in the motor domain. (S)-monastrol, as compared to the (R)-enantiomer, is a more potent inhibitor of Eg5 activity in vitro and in vivo. As Monastrol, by specifically inhibiting kinesin Eg5, can cause mitotic arrest and monopolar spindle formation, it exhibits antitumor properties. Monastrol has being shown to be a potent inhibitor of pteridine reductase (PTR1) in Leishmania; it inhibits proliferation of amastigotes with an IC(50) (50% inhibitory concentration) of 10 uM in macrophage cultures infected with an L. donovani clinical isolate, with no host cytotoxicity. In experimental animals, oral administration of a 5 mg/kg dose of monastrol on two alternate days inhibits 50% of parasite growth, giving therapeutic backing to the use of monastrol as a potent antileishmanial in human VL cases.

Crocetin gentiobiosylglucosyl ester (Crocin II) is extracted from saffron (Crocus sativus L.). Tricrocin is a water soluble crocetin glycoside, a carotenoid pigment of saffron (Crocus sativus L.) that has been used as a spice for flavoring and coloring food preparations, and in Chinese traditional medicine as an anodyne or tranquilizer. Saffron is now used worldwide in folk medicine and is reputed to be useful in treating various human disorders such as heart and blood disorders. Stroke and heart attack are involved in reputed folkloric uses of saffron. Saffron is orally administrated as a decoction. Saffron extract exerts a protective effect on renal ischemia reperfusion induced oxidative damage in rats; Crocetin esters present in saffron stigmas and in Gardenia jasminoides Ellis fruit are the compounds responsible for their color. Crocin, in general term, includes Crocin-I (Crocetin-di-beta -D-gentiobiosyl ester), Crocin-II (Crocetin-beta-D-gentiobiosyl-beta-D-glucosyl ester), Crocin-III (Crocetin-mono-beta-D-gentiobiosyl ester), Crocin-IV (beta-D-monoglucoside ester of monomethyl alpha-crocetin). Saffron from Zhejiang (containing 21.15 ug/ml of Crocetin gentiobiosylglucosyl ester) has significant antitumor effects in vitro and in vivo through caspase-8-caspase-9-caspase-3 mediated cell apoptosis. It thus appears to have a potential as a therapeutic agent.

1,25-dihydroxycalciferol (1,25-dihydroxyvitamin D2 or ercalcitriol) is a metabolite of vitamin D. It exerts antirachitic activity in animals. 1,25-dihydroxycalciferol and its analogs have antineoplastic actions in vitro.

NU6102 is a potent CDK1/cyclin B and CDK2/cyclin A3 inhibitor (IC50 values are 9.5 and 5.4 nM for CDK1/cyclin B and CDK2/cyclin A3 respectively). Antiproliferative agent. Induces G2/M cell cycle arrest. Shows antitumor effects in vivo. NU6102 and its prodrug NU6301 have pharmacological properties consistent with CDK2 inhibition, and represent useful tool molecules for the evaluation of CDK2 as a target in cancer.

Isovitexin (apigenin-6-C-glucoside), an isomer of vitexin, is found in plants such as pigeon pea, Passiflora, bamboo, mimosa, wheat leaves, rice hull of Oryza sativa and others. Isovitexin is poorly absorbed in the gastrointestinal tract. The highest level of intravenously administrated isovitexin was examined in kidney, liver, lung, and lowest in the brain. Isovitexin helps to stimulate apoptotic cell death and autophagy of various cancer cells through the upstream regulation of Bax, PARP, p-JNK, and MAPK and the downstream regulation of the caspases Bcl-2 and ERK1/2. Isovitexin has been proved to have various activities, such as anti-oxidant, anti-inflammatory, anti-Alzheimer's disease and others.