U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1021 - 1030 of 18894 results

Status:
Investigational
Source:
NCT01610388: Phase 1 Interventional Completed Infections, Bacterial
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LANOPEPDEN is an inhibitor of peptide deformylase, a bacterial enzyme required for protein maturation. It was in development for the treatment of complicated bacterial skin infection and hospitalized community-acquired pneumonia.
Status:
Investigational
Source:
NCT00522652: Phase 1 Interventional Completed Advanced Solid Tumors
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



PX-478 is a highly potent and selective Hypoxia-inducible Factor-1α (HIF-1α) inhibitor. It lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. Its inhibition is independent of the tumor suppressor genes VHL and p53, and may be related to derangements in glucose uptake and metabolism due to inhibition of glucose transporter-1 (Glut-1). PX-478 has excellent activity against established human tumor xenografts, inducing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. In high-fat-diet mice, PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. PX-478 had been in phase I clinical trials by for the treatment of lymphoma and solid tumors. However, this research has been discontinued.
Status:
Investigational
Source:
NCT00861549: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Phencynonate (PHH) is a novel anticholinergic compound. It is structurally similar to scopolamine, possesses both muscarinic and nicotinic antagonistic properties as well as anti-NMDA properties. It has been developed as a safe and effective drug for the prevention of motion sickness in tablet form, it also demonstrates clear anticonvulsant effectiveness after soman poisoning in a rat model. S-isomer was more effective against motion sickness and had not anxiogenic action at therapeutic doses. S-isomer has the higher affinity and activity for mAChR in cerebral cortex and acted as a competitive mAChR antagonist. PHH was able to suppress chronic unpredictable mild stress (CUMS)-induced oxidative stress and enhance the antioxidant capacity and antioxidant proteins activity, such as superoxide dismutase 2 (SOD2) and peroxiredoxin 6 (Prdx6). PHH ameliorated CUMS-induced depressive phenotypes by up-regulating SIRT6 deacetylation activity. PHH-mediating SIRT6 pathway is required for antidepressant response and PHH can be used as a novel therapeutic to effectively treat depression. Phencynonate is in phase III clinical trials for the treatment of vertigo.
Status:
Investigational
Source:
NCT00475683: Phase 3 Interventional Completed Chemotherapy Induced Mucositis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Curcumol is one of the major components of the essential oil of Rhizome Curcumae with the structure of sesquiterpenoid hemiketal. It exhibits characteristics such as antitumor, ant proliferation, anti-inflammatory, anti-hepatic fibrosis, antioxidant, and antimicrobial activities with low cytotoxicity. Curcumol suppresses the Breast Cancer Cells, Colorectal Cancer Cell Line, lung adenocarcinoma cell lines and others. However, its effect and mechanisms against tumor metastasis are still unclear. Recently was discovered a preliminary mechanism the suppression of breast cancer cell metastasis by curcumol. This mechanism suggested the inhibition of MMP-9 via JNK1/2 and Akt (Ser473)-dependent NF-κB signaling pathways.
Status:
Investigational
Source:
INN:vinburnine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02415439: Phase 1 Interventional Completed Healthy
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02202447: Phase 1 Interventional Completed Prostate Cancer
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00139672: Phase 2 Interventional Completed Irritable Bowel Syndrome
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PD-217014 or PD-217,014, a new GABA analog was developed by Pfizer as a potent alpha(2)delta ligand of voltage-gated calcium channel, that and possessed visceral analgesic activity. This compound was undergoing phase II clinical trials for the treatment of overactive bladder (OAB) and irritable bowel syndrome (IBS). In addition, PD-217014 was investigated for postherpetic neuralgia treatment. However, all these studies were discontinued.
Status:
Investigational
Source:
NCT02666001: Phase 1 Interventional Completed Infection, Human Immunodeficiency Virus
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Norbuprenorphine is a major metabolite of buprenorphine and potent agonist of μ, δ, and κ opioid receptors. Norbuprenorphine is the only known active metabolite of buprenorphine. It has been shown to be a respiratory depressant in rats, but only at concentrations at least 50-fold greater than those observed following application to humans of BuTrans 20 mcg/h. Compared with buprenorphine, norbuprenorphine causes minimal antinociception but greater respiratory depression. In rats, nor-buprenorphine had 1/50th the analgesic potency of buprenor-phine but 10-fold greater respiratory depressant potency. Norbuprenorphine is an in vitro substrate of the efflux transporter P-glycoprotein (Mdr1). Norbuprenorphine is an in vitro and in vivo substrate of P-glycoprotein. P-glycoprotein-mediated efflux influences brain access and antinociceptive, but not the respiratory, effects of norbuprenorphine.
Status:
Investigational
Source:
NCT03765983: Phase 2 Interventional Active, not recruiting Breast Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Showing 1021 - 1030 of 18894 results