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β-peltatin-β-D-glucopyranoside is a cytotoxic compound which can be extracted from the terrestrial plant Bridelia ferruginuea and Cleistanthus boivinianus. β-peltatin-β-D-glucopyranoside has attracted attention as a potential scaffold for the development of new anticancer compounds.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Elaiophylin (also known as Azalomycin-B) is a natural compound, a macrolide antibiotic that was first isolated from a culture of Streptomyces melanosporus. Elaiophylin is a novel and potent inhibitor of late-stage autophagy with outstanding antitumor activity in human ovarian cancer cells. In addition was shown, that elaiophylin could be a promising therapeutic strategy for overcoming incurable multiple myeloma (MM), even when TP53 mutations are present. It is known, that autophagy inhibition is a promising approach and is being investigated as a new target strategy for ovarian cancer treatment. Autophagy, a lysosome-dependent pathway, is a complex catabolic process that involves the degradation of dysfunctional or useless cytoplasmic constituents. Thus, elaiophylin, a novel autophagy inhibitor with unique chemical structure, provides the potential for structure-based development of autophagy inhibitors for new cancer therapies. Also, elaiophylin is an inhibitor of a testosterone 5 alpha-reductase.
Emodin-8-O-beta-D-glucoside extracted from the traditional Chinese medicinal herb Polygonum cuspidatum Sieb. et Zucc, which is used to treat fractures, rheumatoid arthritis, muscle injury and pain possible by antioxidative mechanism. Emodin-8-O-beta-D-glucoside can be a promising antitumor agent for cancer treatment, because experiments with cervical cancer SKOV3 cells have shown, that it can inhibit the proliferation of cells and promote apoptosis by down regulation of Bcl-2 expression and up regulation of Bax expression, as well as the increase of relative activity of caspase 3 and caspase 9. In addition, emodin-8-O-beta-D-glucoside is able to provide neuroprotection against cerebral ischemia-reperfused injury and glutamate induced neuronal damage through exerting antioxidative effects and inhibiting glutamate neurotoxicity.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
S-Allylcysteine (SAC), the most abundant organosulfur compound in aged garlic extract, has multifunctional activity via different mechanisms and neuroprotective effects that are exerted probably via its antioxidant or free radical scavenger action. Anticancer effects of SAC were reported in prostate cancer, breast cancer, oral cavity cancer, non-small cell lung cancer, neuroblastoma, and hepatocellular carcinoma through the restoration of E-cadherin, the reduction of Slug and matrix metalloproteinase (MMP) protein expression, and stimulating apoptotic pathways. In addition, recently was revealed, that SAC might have imperative implications for the deterrence and early treatment of type 2 diabetes by reducing the influx of glucose in the polyol pathway, thereby elevating the GSH level and reducing the activities of aldose reductase (AR) and sorbitol dehydrogenase (SDH).
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
5-Fluoroorotic acid is a fluorinated derivative of the pyrimidine precursor orotic acid. 5-Fluoroorotic acid exert considerable antitumor activity against transplanted tumors in rats and mice. 5-Fluoroorotate shows increased cytotoxicity on ovarian carcinoma cell lines following encapsulation in liposomes. 5-Fluoroorotic acid is used in vitro in the positive selection of genetically transformed yeast cells.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Aloesin is a chromone derivative isolated from aloe vera. It has many biological effects, such as wound and burn healing properties, and antioxidant, free radical scavenging, anti-inflammatory, and immunomodulatory effects. Aloesin has been shown to be a potent and selective inhibitor of tyrosinase. It exhibited direct inhibitory effects on melanogenesis. Aloesin treatment showed pigmentation suppression in a dose-dependent manner. Thus, aloesin may be used as an agent that inhibits melanin formation induced by UV radiation. Aloesin is thought to be one of the active ingredients in regards to the anti-diabetic activity of Aloe. Aloesin exerts its anticancer effect through the MAPK signaling pathway. It is a novel therapeutic drug for ovarian cancer treatment.
Status:
US Previously Marketed
Source:
AMIFOSTINE by EUGIA PHARMA SPECLTS
(2017)
Source URL:
First approved in 1995
Source:
ETHYOL by COSETTE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Amifostine is an organic thiophosphate cytoprotective agent known chemically as 2-[(3¬ aminopropyl)amino]ethanethiol dihydrogen phosphate (ester), it’s adjuvant used in cancer chemotherapy and radiotherapy involving DNA-binding chemotherapeutic agents. It is marketed under the trade name Ethyol. Amifostine is a prodrug and is dephosphorylated by alkaline phosphatase in tissues to a pharmacologically active free thiol metabolite. This metabolite is believed to be responsible for the reduction of the cumulative renal toxicity of cisplatin and for the reduction of the toxic effects of radiation on normal oral tissues. The ability of Ethyol to differentially protect normal tissues is attributed to the higher capillary alkaline phosphatase activity, higher pH and better vascularity of normal tissues relative to tumor tissue, which results in a more rapid generation of the active thiol metabolite as well as a higher rate constant for uptake into cells. The higher concentration of the thiol metabolite in normal tissues is available to bind to, and thereby detoxify, reactive metabolites of cisplatin. This thiol metabolite can also scavenge reactive oxygen species generated by exposure to either cisplatin or radiation. Healthy cells are preferentially protected because amifostine and metabolites are present in healthy cells at 100-fold greater concentrations than in tumor cells.
Status:
US Previously Marketed
Source:
D B I by CIBA
(1961)
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It activates AMP-activated protein kinase (AMPK) and inhibits mTORC1 signaling. Phenformin used for the treatment of diabetes. Phenformin was removed from the U.S. market 20 years ago because of a high incidence of lactic acidosis. Risk factors for the development of lactic acidosis include renal deficiency, hepatic disease, cardiac disease, and drug interaction such as cimetidine. Phenformin exerts potential anti-neoplastic action.
Status:
US Previously Marketed
Source:
Ammoniated Glycyrrhizin U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Ammoniated Glycyrrhizin U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Glycyrrhizic Acid is specific compound isolated from licorice plants. Ammonium Glycyrrhizate (also known as GLYCYRRHIZIN, AMMONIATED) is a salt, was investigated to be a safe and is used as ingredient in the formulation of makeup, fragrance, hair care, skin care, shaving, personal hygiene and suntan products.
Status:
Possibly Marketed Outside US
Source:
21 CFR 352
(2016)
Source URL:
First approved in 2016
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Lysophosphatidic acid (LPA) is a multifunctional intercellular phospholipid messenger. LPA stimulates the growth of a variety of cells including fibroblasts, vascular smooth muscle cells, endothelial cells, and keratinocytes. It is produced in relatively high levels from activated platelets and can be detected in bodily fluids including serum, saliva, follicular fluid, and malignant effusions. LPA acts as a proliferative and anti-apoptotic factor and is a ligand for LPA1 (EDG-2), LPA2 (EDG-4) and LPA3 (EDG-7) receptors. The plasma LPA level can be a useful marker for ovarian cancer, particularly in the early stages of the disease. It is known, that the therapeutic administration of LPA also blocked APAP-induced liver damage, leading to an increased survival rate by increasing the glutathione level but decreasing inflammatory cytokines in an LPA1,3,5-independent manner. Thus, LPA might be an important therapeutic agent for drug-induced liver injury. In addition, was shown, that LPA levels in plasma and ascites may be useful diagnostic biomarkers for peritoneal carcinomatosis of gastric cancer.