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Restrict the search for
m nalidixic acid
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Mofarotene is an analog of retinoic acid patented by a Swiss multinational healthcare company Hoffmann-La Roche as neoplasm inhibitors and agent for treating dermatoses. Like other retinoic acid agents, mofarotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. Mofarotene has demonstrated considerable antitumor activity in a number of cancer cell lines. Mofarotene in combination with cisplatin and etoposide was studied in phase I clinical trials but further development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Aconiazide, the isonicotinylhydrazone of 2-formylphenoxyacetic acid, has been used in the treatment and prophylaxis of tuberculosis. Aconiazide is a pro-drug of isoniazid which was designed to be less toxic than the parent drug. Aconiazide is hydrolyzed in the body to isoniazid and 2-formylphenoxyacetic acid. 2-Formylphenoxyacetic acid has been shown to bind hydrazine and acetylhydrazine. This binding could explain the lower toxicity of aconiazide and also could provide a reason for postulating its lack of carcinogenicity.
Class (Stereo):
CHEMICAL (ACHIRAL)
Sulotroban is a phenoxyalkylcarboxylic acid derivative patented by Boehringer Mannheim G.m.b.H. as thrombocyte aggregation inhibitor and lipid-lowering agent. Sulotroban is the first thromboxane A2 receptor antagonist available for use in man. Its antagonistic profile appeared to be specific and competitive both for platelets and vascular or bronchial smooth muscle receptors. In preclinical models Administered as a single dose of 800 mg, sulotroban antagonized arachidonic acid-induced, collagen-induced, and U-46619-induced platelet aggregation. In clinical trials, Sulotroban shows superior efficacy to placebo in preventing acute problems during, or restenosis after, coronary angioplasty. Chronic dosage with the drug did not lead to any accumulation of its blocking effect on platelet function; the effect of each dose declined to zero 6-7 hours after dosing.
Status:
Investigational
Source:
NCT00004431: Not Applicable Interventional Completed Trigeminal Neuralgia
(1998)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
(S)-baclofen (or L-baclofen) is an enantiomer of baclofen, a direct GABA-B receptor mimetic. L-baclofen represents a significant improvement over racemic baclofen in the treatment of trigeminal neuralgia.
Status:
Investigational
Source:
NCT00234169: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00505076: Phase 2 Interventional Completed Schizophrenia
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
MK 0777 is a selective GABAA α2/3 receptor partial agonist, for potential use in the treatment of Schizophrenia, Anxiety Disorder, and Generalized Anxiety Disorder. MK-0777 is functionally selective for the α2 and α3 subunits, with virtually no activity for the α1 and α5 subunits. Therefore, MK-0777 cause less sedation, interact less with alcohol, and exhibit less abuse potential and physical dependence than benzodiazepines. Unfortunately, in clinical trials, MK-0777 has little benefit for cognitive impairments in people with schizophrenia and anxiety disorder.
Status:
Investigational
Source:
NCT00691132: Phase 2 Interventional Completed Lung Cancer
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Phenethyl isothiocyanate (PEITC) presents in cruciferous vegetables which have been shown to decrease the risk of various types of malignancies. PEITC targets multiple proteins to suppress various cancer-promoting mechanisms such as cell proliferation, progression and metastasis. PEITC induces apoptosis in human colon cancer HT-29 cells, prostate cancer cells, and osteogenic sarcoma U-2 OS cells. Unique to prostate cancer is that PEITC downregulates the transcriptional factor Sp1, a regulator of AR expression. PEITC suppresses 4-(methylnitrosamino)-1-(3-pyridyl)-1-butoneinduced pulmonary neoplasia in A/J mouse lung, exhibits cancer chemopreventive activity in rat and reduces azoxymethane-induced colonic aberrant crypt foci formation. PEITC appears to be a promising agent for cancer therapy and is already under clinical trials for leukemia and lung cancer.
Status:
Investigational
Source:
NCT00290953: Phase 2/Phase 3 Interventional Completed Lung Cancer
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Meclinertant (SR-48692) is the first non-peptide antagonist of neurotensin receptors. It is potent and selective vs the high-affinity binding sites and with a small activity on the levocabastine-sensitive binding sites. It is active on several species including man without partial agonist properties. In vivo, it is active by oral route with a long duration of action and it is able to cross the blood-brain barrier. Meclinertant may be considered a powerful tool for investigating the role of neurotensin in physiological and pathological processes. Meclinertant has been developing for the treatment of anorexia nervosa; colorectal cancer; irritable bowel syndrome; pain; pancreatic cancer; prostate cancer; schizophrenia; small cell lung cancer however its development was discontinued.
Status:
Class (Stereo):
CHEMICAL (EPIMERIC)
Ciclotropium is quaternary ammonium compound with anticholinergic and parasympatholytic activity. Oral Cyclotropium bromide inhibited fasting and meal-stimulated colonic motility significantly without causing adverse side effects. After cyclotropium bromide, there was a significant correlation between antral contraction amplitude and gastric emptying.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Ormaplatin (NSC 363812, tetraplatin) is a stable platinum (IV) analog. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. Ormaplatin showed marked
antitumor activity both in vitro and vivo. The severe, cumulative and irreversible peripheral neurotoxicity observed in phase I studies resulted in termination of further clinical development of ormaplatin.
