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

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Showing 31231 - 31240 of 34988 results

Status:
Designated
Source:
FDA ORPHAN DRUG:599417
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Designated
Source:
EU-Orphan Drug:EU/3/18/2055
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Designated
Source:
FDA ORPHAN DRUG:515216
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Designated
Source:
EU-Orphan Drug:EU/3/14/1242
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


F-15599 is a novel agonist with high selectivity and efficacy at serotonin 5-HT(1A) receptors. In signal transduction, electrophysiological and neurochemical tests, F-15599 preferentially activates post-synaptic 5-HT(1A)Rs in rat frontal cortex. Such a profile may translate to an improved profile of therapeutic activity for mood disorders. [(18)F]F-15599 is a radiofluorinated agonist presenting interesting characteristics for probing in vitro and in vivo the high-affinity states of the 5-HT(1A) receptors. The Rett Syndrome Research Trust awarded a grant to Neurolixis to advance F-15599 to clinical development.
Aphidicolin, a tetracyclic diterpenoid obtained from the culture filtrates of Cephalosporium aphidicola and other fungi, inhibits the growth of eukaryotic cells and of certain animal viruses (SV40, Herpes and Vaccinia viruses) by selectively inhibiting the cellular replicative DNA polymerase alpha or the viral-induced DNA polymerases. The arrest of cellular or viral growth is thus due to inhibition of cellular or viral replicative DNA synthesis without interference with mitochondrial DNA synthesis, RNA, protein and nucleic acid precursors synthesis or other major metabolic pathways. The inhibition of all sensitive eukaryotic DNA polymerases by aphidicolin is competitive with respect to dCTP. Aphidicolin has thus proved extremely useful in elucidating the functional role of DNA polymerase alpha in nuclear DNA replication, of DNA polymerase gamma in mitochondrial DNA synthesis and both DNA polymerases beta and alpha in DNA repair synthesis. An important laboratory application of aphidicolin is the synchronization of the cell cycle of eukaryotic cells both in culture and in vivo. The properties of aphidicolinhave recently aroused considerable interest for its possible exploitation in al practice. The mechanism of action of this drug suggests in fact that it may be useful for controlling excessive cell proliferation in patients with cancer, psoriasis or other dermatitis with little or no adverse effect upon non-multiplying cells.
Boldine, an aporphine alkaloid, found abundantly in the leaves/bark of boldo (Peumus boldus Molina) widely consumed in the folk medicine of some regions. Boldine possesses various pharmacological properties including, anticancer activity. It exhibits a significant improvement of learning and memory through inhibition of brain acetylcholinesterase activity and alleviation of brain oxidative stress, which was shown on animal models. Boldine is a potentially useful agent for the treatment of leishmaniosis. In addition, it suppresses osteoclastogenesis, improves bone destruction and may be a potential therapeutic agent for rheumatoid arthritis. Besides, was shown, that boldine inhibits telomerase in cells treated with sub-cytotoxic concentrations. Telomerase inhibition occurs via down-regulation of human telomerase reverse transcriptase (hTERT), the catalytic subunit of the enzyme.
Status:
Designated
Source:
FDA ORPHAN DRUG:550316
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

APC-3316 is a vinyl sulfone cystein protease inhibitor. It is a potent, irreversible cysteine protease inhibitor and a potent and selective CCR4 antagonist. Its therapeutic targets are cruzain, a cysteine protease of the protozoan parasite Trypanosoma cruzi, and cathepsins B and L, which are associated with cancer progression. It was discontinued after preclinical trials in Chagas disease in USA.
Status:
Designated
Source:
FDA ORPHAN DRUG:550316
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

APC-3316 is a vinyl sulfone cystein protease inhibitor. It is a potent, irreversible cysteine protease inhibitor and a potent and selective CCR4 antagonist. Its therapeutic targets are cruzain, a cysteine protease of the protozoan parasite Trypanosoma cruzi, and cathepsins B and L, which are associated with cancer progression. It was discontinued after preclinical trials in Chagas disease in USA.
Status:
Designated
Source:
FDA ORPHAN DRUG:169303
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

NSC-631570 (Ukrain) is a semisynthetic compound of thiophosphoric acid and the alkaloid chelidonine from the plant Chelidonium majus. Ukrain was promoted as a drug to treat cancer and viral infections, including HIV and hepatitis. It exerts a selective cytotoxic effect on tumor cells in vitro and in vivo and shows the ability to modulate immunocyte functions. Ukrain has been used in complementary herbal medicine for more than 20 years for the treatment of benign and malignant tumors. Thus, in unresectable advanced pancreatic cancer, Ukrain alone and in combination with gemcitabine nearly doubled the median survival times in patients suffering from advanced pancreatic cancer. Inhibition of the growth of cancer cell lines in vitro, tumor mass reductions in vivo, and partial and complete remissions in oncological patients, occur as a result of Ukrain application. The drug may interfere directly with the metabolism of cancer cells and it also improves the functioning of the host immune system. Diminished synthesis of DNA, RNA and proteins, the inhibition of cellular oxygen consumption, and the induction of programmed cell death in malignant cells have been described following Ukrain administration. The drug can also modify the immunological response via an increase in the number of total T-cells and a normalization of the T-helper/T-suppressor lymphocyte ratio. However,according to the American Cancer Society and the Memorial Sloan-Kettering Cancer Center, there is no evidence that Ukrain is an effective cancer treatment. Through an Austrian company known as Nowicky Pharma, the drug, which was never approved by regulators, was sold as a treatment for AIDS, radiation-induced diseases and as a cure for all forms of cancer. Ukrain is not approved by the Food and Drug Administration but is available in parts of Europe and from Tijuana clinics.
Status:
Designated
Source:
FDA ORPHAN DRUG:478615
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Showing 31231 - 31240 of 34988 results