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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
BROTIANIDE is salicylanilide derivative used to treat fascioliasis in sheep. A dose of 7 mg/kg of brotianide shows 91-99% activity against 7-14 weeks old flukes; however, its activity against 6 weeks old flukes is weak (50-90%). It also possesses 85-90% activity against paramphistomes in sheep and cattle. The maximum tolerated dose of brotianide is 27 mg/kg in sheep.
Class (Stereo):
CHEMICAL (ACHIRAL)
Bromoxanide shows high activity against 6-week-old worms of F. hepatica and the nematode Hae- monchus contortus at very low doses.
Status:
Investigational
Source:
NCT01357395: Phase 2 Interventional Completed Small Cell Lung Carcinoma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Amuvatinib (formerly known as MP470) is an oral multi-targeted tyrosine kinase inhibitor, which play critical roles in transducing growth signals to cancer cells. It suppresses c-MET, c-RET and the mutant forms of cKIT, PDGFR and FLT3. It also disrupts DNA repair likely through suppression of homologous recombination protein Rad51, an important survival pathway in many human cancers. In vitro and in vivo data have demonstrated amuvatinib synergy with DNA damaging agents including etoposide and doxorubicin. Overall, in the amuvatinib clinical development program, over 200 subjects were exposed to at least one dose of amuvatinib. In the Phase 1b clinical study in combination with carboplatin and etoposide, responses in small cell lung cancer (SCLC), neuroendocrine as well as other tumor types were observed. Human pharmacokinetic data suggest that co-administration of amuvatinib did not alter exposures of standard of care agents including carboplatin, etoposide, doxorubicin, paclitaxel, topotecan or erlotinib as measured by overall exposure. In the first-in-human study, durable clinical benefit was observed in the gastrointestinal stromal tumors (GIST) with modulation of Rad51 observed in skin punch biopsies. In clinical trials, amuvatinib has demonstrated a wide therapeutic window and shows minimal toxicity in the expected therapeutic dose range, despite suppressing several signaling pathways within cells. However, in spite of this, this drug was discontinued, because it was not pre-specified primary endpoints in the clinical proof of concept (cPOC) stage. But the combination of MP470 and Erlotinib, which target the HER family/PI3K/Akt pathway may represent a novel therapeutic strategy for prostate cancer.
Status:
Investigational
Source:
NCT01214603: Phase 2 Interventional Completed Leukemia
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
LY-2090314 is a GSK-3alpha and GSK-3beta inhibitor developed by Eli Lilly. Phase 2 clinical trials of LY-2090314 as a signle agenst against acute leukemia did not show clinical benefit. LY-2090314 was studied in combination pemetrexed and carboplatin against solid tumors, and in combination with FOLFOX, gemcitabine, and nab-paclitaxel against pancreatic cancer.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Clazuril is benzene-acetonitrile derivative, developed by Janssen Pharmaceutica as an anticoccidial agent for the treatment of pigeons. The anticoccidial effect is due to a cidal effect on the endogenous stages of the Eimeria species.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Lufironil (HOE 077) is an inhibitor of prolyl 4-hydroxylase. In preclinical studies, it prevented liver fibrosis by inhibiting not only the hydroxylation of proline but also the activation of Ito cells, which are considered the main collagen-producing cells, resulting in reduced expression of procollagen mRNA. Lufironil was being developed for the treatment of chronic liver diseases including alcoholic hepatitis and liver cirrhosis.
Class (Stereo):
CHEMICAL (RACEMIC)
Loviride (R 89439) is a non-nucleoside inhibitor of reverse transcriptase. It inhibits virion and recombinant reverse transcriptase of HIV-1. It was being studied in the combination therapy of HIV infection with other anti-HIV agents.
Status:
Investigational
Source:
NCT03598309: Phase 2 Interventional Recruiting Lung Diseases
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Demethoxycurcumin is a derivative or curcumin and represents one of the major active components of curcumin products isolated from Curcumae sp. In preclinical models, Demethoxycurcumin inhibits LPS-induced nitric oxide (NO) production, and expression of iNOS and COX2 in RAW264.7 cells by blocking NF-kB activation. Demethoxycurcumin also inhibits NF-kB dependent iNOS, TNFα and IL-1β expression in LPS-treated rat microglial cells. Demethoxycurcumin suppresses the expression of MMPs and ICAM-1 in MDA-MB-231 human breast cancer cells by inhibition of NF-kB. Demethoxycurcumin is currently in Phase I clinical trials.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Piprofurol is a benzofuran chalcon derivative. It is a calcium channel blocker. Piprofurol inhibited in a concentration-dependent manner the calcium-induced contractions in isolated potassium depolarized preparations of rat aorta and relaxed the K+-induced contraction of the dog coronary artery and the rabbit basilar artery. Piprofurol also inhibited noradrenaline-induced vascular smooth muscle contractions but the antagonism was clearly noncompetitive and the contractions induced were altered by concentrations two orders of magnitude higher than the concentration inhibiting calcium-induced contractions. Piprofurol exerts a negative inotropic effect on guinea-pig papillary muscle. These effects suggested a potentially anti-ischemic activity. This is confirmed in anaesthetized dogs, where piprofurol reduced the epicardial ST-segment elevation following coronary artery occlusion, and in isolated heart preparations, where it decreased the leakage of LDH during periods of anoxia and reoxygenation. Piprofurol is a coronary vasodilator and antihypertensive agent.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ditekiren is a relatively large renin inhibitor incorporating the hydroxyethylene isostere as well as both the P4 proline and P2’ isoleucine of angiotensinogen. Methylation of the P2-site histidine backbone nitrogen stabilizes the P2-P3 peptide bond towards degradation by chymotrypsin. Even though oral bioavailability was low, serum ditekiren levels were equivalent to 4–8 times the in vitro IC50 for renin inhibition for this peptide throughout the 2.5 h after oral administration that blood levels were monitored. In Na-depleted cynomolgus monkeys, oral dose elicited a hypotensive response that had not returned to baseline by 5 h. Ditekiren had been in phase II clinical trials for the treatment of heart failure and hypertension. However, these studies were discontinued.
