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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
NCT00337389: Phase 3 Interventional Unknown status Metastatic Colorectal Cancer
(2006)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Targets:
Folitixorin, a thymidylate synthase inhibitor is a substrate used by the enzyme methylenetetrahydrofolate reductase (MTHFR) to generate 5-methyltetrahydrofolate. Folitixorin was studied in clinical trials for the treatment of breast cancer, metastatic colorectal cancer and for the treatment of advanced pancreatic cancer. Folitixorin had been granted orphan drug status for the treatment of pancreatic cancer in both the U.S. and EU. However, further development of this drug was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Clantifen is an aminothiophene derivative invented by Hoersht AG. The compound is claimed to have antiphlogistic and antipyretic properties.
Class (Stereo):
CHEMICAL (ACHIRAL)
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
Source:
NCT03762031: Phase 1 Interventional Completed Healthy
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
M40419 (now GC4419) is a Mn(II)-containing pentaazamacrocyclic selective superoxide dismutase mimetic. It is a first-in-class, small molecule enzyme mimetic that converts superoxide to hydrogen peroxide and molecular oxygen. GC4419 is currently being evaluated in an ongoing randomized Phase 2 clinical trial to assess its effect on the incidence, severity and duration of severe oral mucositis (OM) when given to patients with squamous cell cancers of the head and neck in combination with radiation and chemotherapy. GC4419 has received Breakthrough Therapy and Fast Track designations from the U.S. Food and Drug Administration.
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.
Class (Stereo):
CHEMICAL (ACHIRAL)
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.
