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Restrict the search for
beta carotene
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Netivudine [882C, 882C87, BW 882, Py-araU, Zonavir®] is an orally active thymidine analogue which was being investigated as a treatment for herpes zoster virus infections. Netivudine is a nucleoside analog with potent, specific activity against varicella-zoster virus. It is approximately seven times as potent as acyclovir with an in vitro 50% inhibitory concentration of 1 to 2 uM.
Class (Stereo):
CHEMICAL (ACHIRAL)
Nitromiphene (NIT; CI 628) is a triarylethylene antiestrogen shown to be effective in treatment of experimental breast cancer. Nitromiphene is one of the earliest nonsteroidal selective estrogen receptor modulators (SERMs). It is an anti-estrogen capable to translocate the estrogen receptor to the nucleus and to induce the replenishment of the cytosol receptor. Nitromiphene inhibited the uptake of [3H]-estradiol in rat whole homogenates and isolated cell nuclei tissues and the pituitary, and inhibited estradiol-induced female sexual behavior. Nitromiphene has thus been shown to suppress the growth of chemically induced and ransplantedmammary tumors in rodents. Also, Nitromiphene was shown to have potent, prolonged antiuterotropic effects in immature rats. Nitromiphene has been shown to undergo conversion to demethyl Nitromiphene (CI628M), a phenolic metabolite which had greater affinity for estrogen receptors and greater biological potency in vitro than did Nitromiphene. However, the in vivo antiestrogenic effects of Nitromiphene and demethyl Nitromiphene were similar, possibly due to facile O-demethylation of the former compound after administration.
Status:
Investigational
Source:
NCT00346502: Phase 1/Phase 2 Interventional Withdrawn Dysplastic Nevus Syndrome
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Betulinic acid (BA) is a plant-derived pentacyclic triterpenoid that exerts potent anti-cancer effects in vitro and in vivo. It`s anticancer property is linked to its ability to induce apoptotic cell death in cancer cells by triggering the mitochondrial pathway of apoptosis. In contrast to the cytotoxicity of betulinic acid against a variety of cancer types, normal cells and tissue are relatively resistant to betulinic acid, pointing to a therapeutic window. Compounds that exert a direct action on mitochondria present promising experimental cancer therapeutics, since they may trigger cell death under circumstances in which standard chemotherapeutics fail. Thus, mitochondrion-targeted agents such as betulinic acid hold great promise as a novel therapeutic strategy in the treatment of human cancers. Betulinic acid has antiretroviral, antimalarial, and anti-inflammatory properties. Betulinic acid exerts its inhibitory effect by preventing topoisomerase I-DNA interaction as a result of which the 'cleavable complex' is not formed. In consequence, it also acts as an antagonist to camptothecin-mediated cleavage. The antitumor pharmacological effects of BA consist of triggering apoptosis via the mitochondrial pathway, regulating the cell cycle and the angiogenic pathway via factors, including specificity protein transcription factors, cyclin D1 and epidermal growth factor receptor, inhibiting the signal transducer and activator of transcription 3 and nuclear factor‑κB signaling pathways, preventing the invasion and metastasis of tumor cells, and affecting the expression of topoisomerase I, p53 and lamin B1. Betulinic Acid has also been used in trials studying the treatment of Dysplastic Nevus Syndrome. Betulinic acid acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 uM. Betulinic acid is an inhibitor of HIV-1 with EC50 of 1.4 uM.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ceftiolene (42980RP) is a new cephalosporin with a broad antibacterial spectrum similar to cefotaxime or ceftriaxone. The affinities of ceftiolene for penicillin-binding proteins are very comparable with those of ceftriaxone and cefotaxime for Escherichia coli, and generally greater than those of latamoxef (moxalactam) for the higher molecular weight PBPs of E. coli. Enterobacter cloacae. The affinity of ceftiolene for PBP1 of Staphylococcus aureus is greater than those of cefotaxime or latamoxef but comparable with these antibiotics for PBP3. The bacteriolytic activity of ceftiolene at defined concentrations against Gram-negative organisms is similar to that of ceftriaxone and significantly better than that of the other third-generation cephalosporins tested.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Caprindolol, also known as SDZ 21009, is a beta-adrenoceptor blocker with affinity for serotonin (5-HT1A and 5-HT1B receptors.
Class (Stereo):
CHEMICAL (RACEMIC)
Bometolol is a cardiospecific beta-adrenergic blocking drug that was never marketed.
Status:
Investigational
Source:
NCT00304525: Phase 1/Phase 2 Interventional Completed Metastatic Melanoma
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CHIR-265 (RAF265) is a potent selective orally active small molecule Raf-kinase inhibitor with anti‐angiogenic activity through inhibition of vascular endothelial growth factor type 2 (VEGFR‐2) in preclinical models. CHIR-265 effectively block phosphorylation of Raf's downstream substrates MEK and ERK in cells and also kill melanoma and colorectal cancer cell lines harboring B-Raf mutations independent of PTEN mutation status. Raf kinase inhibition by CHIR-265 in mutant B-Raf melanoma cell lines causes cell cycle arrest and induces apoptosis, mimicking the effect of Raf RNAi in these cells. CHIR-265 also potently inhibits the phosphorylation of VEGFR2 and proliferation of VEGF-stimulated hMVEC.
Status:
Investigational
Source:
INN:dexefaroxan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Dexefaroxan is a selective alpha 2-adrenergic receptor antagonist. Вexefaroxan improved TgCRND8 (protein-transgenic mouse model of Alzheimer's disease) behavioral phenotypes and increased BDNF mRNA expression without affecting amyloid-β peptide levels. Dexefaroxan treatment also enhanced the number and complexity of the dendritic arborizations of polysialated neural cell adhesion molecule-positive neurons. The trophic effects of dexefaroxan on newborn cells might involve an increase in brain-derived neurotrophic factor, which was upregulated in afferent noradrenergic fiber projection areas and in neurons in the granule cell layer. By promoting the survival of new endogenously formed neurons, dexefaroxan treatment represents a potential therapeutic strategy for maintaining adult neurogenesis in neurodegenerative conditions, such as Alzheimer's disease, that affect the hippocampus. Dexefaroxan increases neuron survival in the olfactory bulb of the adult rat in vivo, putatively as a result of reducing the apoptotic fate of telencephalic stem cell progenies.
Status:
Investigational
Source:
JAN:ENZASTAURIN HYDROCHLORIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Enzastaurin is a serine/threonine kinase inhibitor that showed antiangiogenic, antiproliferative, and proapoptotic properties in vitro and antitumor activity in vivo in a xenograft Waldenström macroglobulinemia (WM) model. Enzastaurin (LY317615) is a potent PKCβ selective inhibitor. Enzastaurin suppresses angiogenesis and was advanced for clinical development based upon this antiangiogenic activity. Enzastaurin suppresses tumor growth through multiple mechanisms: direct suppression of tumor cell proliferation and the induction of tumor cell death coupled to the indirect effect of suppressing tumor-induced angiogenesis. Enzastaurin is an orally administered drug that was intended for the treatment of solid and haematological cancers. Enzastaurin had shown encouraging preclinical results for the prevention of angiogenesis, inhibition of proliferation and induction of apoptosis as well as showing limited cytotoxicity within phase I clinical trials. However, during its assessment in phase II and III clinical trials the efficacy of enzastaurin was poor both in combination with other drugs and as a single agent. Eli Lilly discontinued development of enzastaurin after top-line data from the double-blind, international Phase III PRELUDE trial in 758 DLBCL patients showed that enzastaurin missed the primary endpoint of improving DFS vs. placebo.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Epervudine (5-isopropyl-2'-deoxyuridine) is an antiviral compound. The antiviral effect of epervudine on herpes viruses (HSV-1 and HSV-2) is based on the sensitivity of virus DNA to nucleases due to epervudine incorporation into the virus DNA and the resulting change in DNA conformation. Virus selectivity is based on virus induced thymidine kinase activity and on HSV induction of polymerase enzymes catalyzing the incorporation. Epervudine (HEVIZOS) ointment is used to treat herpetic skin infections.
