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

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Showing 391 - 400 of 3145 results

Status:
Investigational
Source:
INN:fosmenic acid
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Fosmenic acid was used for the treatment of atherosclerosis. Information about the current use of this drug is not available.
Lomeguatrib is a O6-methylguanine-DNA-methyl-transferase inhibitor which was developed by AstraZeneca for the treatment of cancer. It was tested in phase I and II of clinical trials for the treatment of colorectal cancer, melanoma and other solid tumors.
Status:
Investigational
Source:
INN:dotarizine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dotarizine was developed as antimigraineur. Dotarizine inhibited the 5-HT2A response in a concentration-dependent manner. The mechanism of blockade by dotarizine of cerebral vessels contractility has three components: (i) presynaptic inhibition of noradrenaline release; (ii) blockade of postsynaptic vascular 5-HT receptors; (iii) blockade of Ca(2+)entry into the vascular smooth muscle cell cytosol. The compound does not affect the vascular receptors for noradrenaline, angiotensin II or prostaglandin F(2alpha). Dotarizine had a pronounced protective effect against electric seizures.
Status:
Investigational
Source:
INN:oxiniacic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Oxiniacic Acid is a nicotinic acid derivative, that shows potent hypolipidemic activity.
Status:
Investigational
Source:
INN:yohimbic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Yohimbinic acid, also known as yohimbic acid is an indole alkaloid, which was isolated from dried roots of Rauwolfia serpentina. Yohimbinic acid is a potent inhibitor of a human DNA Topoisomerase I and can inhibit cancer cells growth.
Status:
Investigational
Source:
NCT00084812: Phase 1 Interventional Completed Unspecified Adult Solid Tumor, Protocol Specific
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Safingol, the synthetic L-threo-stereoisomer of endogenous (D-erythro-) sphinganine, is an inhibitor of protein kinase C and sphingosine kinase in vitro, and in some cell types has been implicated in ceramide generation and induction of apoptosis. Safingol inhibits enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC (IC50 = 37.5 uM and 31uM, respectively). Inhibits human PKCα, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC50 = 40 uM). Safingol enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC) in gastric cancer cells by promoting drug-induced apoptosis. Safingol is an inhibitor of SphK (Sphingosine kinase). Safingol has been shown to act synergistically with other chemotherapeutic agents and may potentiate chemotherapy drug-induced apoptosis in vitro and in vivo.
Status:
Investigational
Source:
INN:salclobuzic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Salclobuzate sodium was developed as an oral absorption promoter. This compound had to “chaperone” poorly permeable payloads across the intestine. Information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT00277810: Phase 2/Phase 3 Interventional Completed Alzheimer Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LECOZOTAN, a benzodioxanylpiperazine derivative, is a selective serotonin 1A receptor antagonist. It was in development for the symptomatic treatment of cognitive deficits in Alzheimer's disease.
Licofelone (ML 3000) is a pyrrolizine derivative originally discovered by Merckle GmbH and developed by EuroAllaince with a unique pharmacological profile, which comprises optimal gastrointestinal tolerability and high analgesic and anti-inflammatory activity. These effects are due to balanced and selective inhibition of both cyclo-oxygenase and 5-lipoxygenase. Inhibition of 5-lipoxygenase may reduce the gastrointestinal toxicity associated with other non steroidal anti-inflammatory drugs, which only inhibit cyclooxygenase. Licofelone also has antipyretic and antiaggregatory properties. Clinical and preclinical trials were also undertaken for osteoarthritis, rheumatoid arthritis, asthma, pain and inflammation. However, development for these indications appear to have been discontinued.
Status:
Investigational
Source:
INN:bensuldazic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Bensuldazic acid was used in veterinary as an antifungal agent.