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Restrict the search for
obeticholic acid
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sinefungin, a natural nucleoside isolated from cultures of Streptomyces incarnatus and S. griseolus, is structurally related to S-adenosylhomocysteine and S-adenosylmethionine. Sinefungin is a DNA methyltransferase (DNMT) inhibitor (IC₅₀ = 0.1 - 20 uM). Sinefungin has been shown to inhibit the development of various fungi and viruses, but its major attraction to date resides in its potent antiparasitic activity. This compound has been reported to display antiparasitic activity against malarial, trypanosomal, and leishmanial species. Sinefungin inhibits pneumococcal biofilm growth in vitro and colonization in vivo, decreases AI-2 production, and downregulates luxS, pfs, and speE gene expressions. Sinefungin was significantly suppressive against both L. donovani and L. braziliensis panamensis infections in hamsters when compared with meglumine antimonate. An immunosuppressed rat model was used to investigate the anti-Cryptosporidium parvum activity of sinefungin. In infected animals, oral sinefungin therapy resulted in a dose-related suppression of oocyst shedding, which correlated with oocyst disappearance from ileal sections. When administered prior to or on the day of oocyst challenge, sinefungin successfully prevented infection. These data suggest that sinefungin could be considered as a candidate molecule in the treatment of human cryptosporidiosis, considered to be the most significant enteric opportunistic infection in AIDS.
Status:
Investigational
Source:
NCT00322140: Phase 1 Interventional Completed Solid Tumors
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
2-Cyano-3,12-dioxooleana-1,9-diene-28-oic acid (CDDO, also known as Bardoxolone) is a synthetic triterpenoid that displays potent anti-inflammatory and antitumorigenic activities. CDDO was in the clinical trial phase I for the treatment patients with Solid tumors and leukemia, but that studies were discontinued. It is known, that CDDO blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2. In addition, was discovered, that CDDO disrupted intracellular redox balance and thereby induce apoptosis. Moreover, CDDO is a ligand for peroxisome proliferator-activated receptor that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Dinaline represents a group of pharmacologically active lipophilic substances with a relatively simple structure derived from N-acyl-o-phenylenediamine. It has been found to exhibit high antineoplastic activity in a series of slowly growing tumors such as chemically induced rat mammary and colorectal carcinomas, osteosarcoma C22LR and Brown Norway myeloid leukemia. The drug was inactive against many of the typically hypersensitive signal tumors, i.e. mouse leukemias P388 and L1210, sarcoma 180 and Yoshida sarcoma. Colon carcinoma cells exposed to dinaline demonstrate distinct but reversible changes in amino acid transport, protein metabolism, DNA synthesis and cell proliferation.
Status:
Investigational
Source:
NCT02226939: Phase 2 Interventional Completed Liver Cirrhosis
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Ciluprevir (BILN-2061) is a selective inhibitor of the HCV NS3 serine protease, which was developed by Boehringer Ingelheim for the treatment of hepatitis C infection. The drug was discontinued in phase II due to adverse events such as cardiac toxicity (demonstrated in animals). In the cell-based replicon assay, ciluprevir inhibited HCV RNA replication at low nanomolar levels. It had inhibitory rate constant (Ki) values of 0.3 and 0.66 nM for the NS3 proteases of HCV genotypes 1a and -1b, respectively.
Status:
Investigational
Source:
INN:metethoheptazine [INN]
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Metethoheptazine (WY-535) is an analgesic agent.
Status:
Investigational
Source:
NCT01086267: Phase 1/Phase 2 Interventional Completed Colorectal Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
BMS-908662 (previously known as XL281) is a small molecule Raf kinase inhibitor that lies immediately downstream of RAS and are key components of the RAS/RAF/MEK/ERK kinase-signaling pathway. Bristol-Myers Squibb has received an exclusive worldwide license to develop and commercialize antineoplastic agent XL281. BMS-908662 participated in phase I development for the treatment of patients with melanoma and in combination with cetuximab for patients with colorectal cancer. However, further, development has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
LANPROSTON is an analog of prostaglandin F2 alpha. It is used as veterinary medicament.
Status:
Investigational
Source:
NCT00458744: Phase 1 Interventional Withdrawn Brain and Central Nervous System Tumors
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Talotrexin (also known as PT-523) was developed as a nonpolyglutamatable antifolate drug for the treatment of various types of tumors. It is known that antifolates are a class of cytotoxic or antineoplastic agents, which inhibit or prevent the maturation and proliferation of malignant cells. Talotrexin was studied in clinical trials for the treatment of brain and central nervous system tumors, leukemia, lymphoma, unspecified childhood solid tumor. However, this study was withdrawn because of toxicity. In addition, was studied in phase I/II multicenter clinical trial in patients with non-small-cell Lung carcinoma, this study was also withdrawn. The withdrawal was related to incidences of dose-limiting mucositis and myelosuppression. However, on May 22, 2006, was announced that the U.S. Food and Drug Administration has granted orphan drug designation for talotrexin in patients with acute lymphoblastic leukemia (ALL).
Class (Stereo):
CHEMICAL (ACHIRAL)
Colfenamate is an antypyretic and antiinflammatory compound developed by the German company Tropon, GmbH.
Status:
Investigational
Source:
NCT00069875: Phase 2 Interventional Completed Carcinoma, Non-Small-Cell Lung
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Etalocib (LY-293111 or VML 295) is a potent and orally active leukotriene B4 receptor antagonist of the biphenylphenol class. It efficiently blocks neutrophil activation and subsequent inflammation. Additionally, it exerts antineoplastic properties through induction of cell cycle arrest and apoptosis in tumor cells. Etalocib was being developed for the treatment of inflammatory diseases and solid tumors.
