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Restrict the search for
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Prinomastat is a synthetic hydroxamic acid derivative with potential antineoplastic activity. Prinomastat inhibits matrix metalloproteinases (MMPs) (specifically, MMP-2, 9, 13, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. As a lipophilic agent, prinomastat crosses the blood-brain barrier. Pfizer conducted multicenter, randomized, double-bind, placebo-controlled trials to evaluate the safety and efficacy of prinomastat in combination with standard chemotherapy in patients with advanced hormone refractory prostate cancer and non-small cell lung cancer. However, this study has been terminated for the reason that Prinomastat did not improve the outcome of chemotherapy in non-small cell Lung cancer patients.
Class (Stereo):
CHEMICAL (ACHIRAL)
Metanixin is an analgesic and anti-inflammatory agent.
Status:
Investigational
Source:
INN:thiacetarsamide sodium [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Thiacetarsamide is a drug containing trivalent arsenic. In the USA it was used for the treatment of Heartworm Infection in dogs and cats under tradename Caparsolate, however, it was discontinued because of the availability of safer alternatives. The mechanism of action for thiacetarsamide is modulation of glucose uptake and metabolism; inhibition of glutathione reductase, and alteration of the structure and function of the surface of the intestinal epithelium of the parasites.
Status:
Investigational
Source:
INN:lomeguatrib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
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
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tizabrin is the antithrombotic, fibrinolytic agent. Tizabrin (CP-2129) stimulates fibrinolysis after intravenous administration in human volunteers due to an increase in tissue plasminogen activator (t-PA) activity. Tizabrin has no intrinsic fibrinolytic activity in vitro.
Status:
Investigational
Source:
NCT01051921: Phase 2 Interventional Completed Hepatitis C
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CTS-1027 (Ro-1130830) is a hydroxamic acid matrix metalloprotease (MMP) inhibitor. CTS-1027 was originally designed as a strong inhibitor of MMP-2, -3, -8, -9, -12, -13 and -14, without inhibiting MMP-1 and MMP-7. CTS-1027 was proved to be safe in clinical trials for osteoarthritis conducted by Roche. CTS-1027 was then licensed from Roche to Conatus Pharmaceuticals and was investigated as a protector from liver fibrosis in hepatitis C virus patients. The development of the drug was discontinued due to laboratory abnormalities and adverse events in a subset of clinical trial participants.
Class (Stereo):
CHEMICAL (ACHIRAL)
Ticolubant (also known as SB-209247) is a pyridine derivative patented by SmithKline Beckman Corp. as an anti-inflammatory leukotriene B4 receptor antagonist. Ticolubant displays high affinity for the human neutrophil LTB4 receptor, blocks LTB4-induced Ca2+ mobilization, and demonstrates potent oral and topical antiinflammatory activity in a murine model of dermal inflammation. However, Ticolubant did not show significant oral activity in a murine model of inflammation. Development of Ticolubant was discontinued when administration to beagle dogs for 28 days was associated with non-dose-dependant inflammatory hepatopathy, with minimal hepatocellular necrosis being observed in the more severe cases
Class (Stereo):
CHEMICAL (EPIMERIC)
KETOTREXATE is an antifolate developed to overcome methotrexate (MTX) resistance. However, it demonstrated such potential only in MTX-resistant sensitive L1210/FR8 leukemia cells and its clinical development was discontinued. Unlike MTX, KETOTREXATE exhibited minimal inhibition of purified dihydrofolate reductase, which implies that it does not act as a classical antifolate.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Lotrafiban (SmithKline Beecham) is a member of the latest generation of orally-active platelet GPIIb/IIIa blockers undergoing Phase III clinical trials to test the relative effectiveness versus other oral platelet inhibitors for ischaemic conditions including unstable angina, restenosis after PCI and stroke. Lotrafiban is converted from an esterified prodrug by plasma and liver esterases to a peptidomimetic of the arginine-glycine-aspartic acid amino acid sequence. This sequence itself mimics the binding site of fibrinogen and von Willebrand Factor to the platelet GPIIb/IIIa receptor. Preliminary results of the clinical trial APLAUD (antiplatelet useful dose) show that lotrafiban is clinically safe and well-tolerated in patients with recent myocardial infarction, unstable angina, transient ischaemic attack (TIA), or stroke when added to aspirin therapy. The Blockade of the IIb/IIIa Receptor to Avoid Vascular Occlusion (BRAVO) trial of SmithKline Beecham's oral GpIIb/IIIa blocker, lotrafiban, has been stopped early because of concerns about both safety and efficacy. The drug was showing a higher mortality rate than placebo, and was also associated with an increased incidence of serious thrombocytopenia and major bleeding. As a result of these findings the company has discontinued development of lotrafiban.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Mureletecan is a water-soluble prodrug, consisting of camptothecin covalently linked to polymeric backbone methacryloylglycynamide, with potential antineoplastic activity. After entering tumor cells, the active moiety camptothecin is slowly released from mureletecan via hydrolysis of the ester linkage. Camptothecin, the active moiety, is an alkaloid isolatable from the Chinese tree Camptotheca acuminata. Camptothecin itself suffers from poor solubility, which is why it is often investigated with a solubilizing conjugate; such as in Mureletecan. Camptothecin binds to and stabilizes the topoisomerase I-DNA covalent complex producing potentially lethal double-stranded DNA breaks when encountered by DNA replication machinery. Camptothecin has also been shown to inhibit HIF1a. Camptothecin has been investigated with a number of solubilizing conjugates as a potential treatment in various forms of cancer.
