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Restrict the search for
methyl salicylate
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
Droxinavir is hydroxyethylurea human immunodeficiency virus type 1 (HIV-1) protease inhibitor. Position 88 of HIV-1 protease gene plays a key role in the interaction between droxinavir and the protease molecule. A mutation in this position, located outside the active site, confers resistance to the hydroxyethylurea inhibitor droxinavir. The V82A and N88S substitutions conferred droxinavir resistance on HIV-1 recombinant variants. Positions 82 and 88 are reported to be variable in natural populations isolated from patients who have not been treated with protease inhibitors. Droxinavir had been in preclinical phase for the treatment of HIV-1 infection. However, this study was discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pinolcaine is 10-methyl-2-substituted piperidine. Pinolcaine is a local anesthetic.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mivobulin is a synthetic water-soluble colchicine analog with the broad antitumor activity that competitively binds tubulin at the colchicine-binding site and inhibits tubulin polymerization. Cancer cells exposed to Mivobulin isethionate accumulate in the M phase of the cell cycle and subsequently die. Preclinical studies have demonstrated that Mivobulin isethionate is able to cross the blood-brain barrier. Importantly, Mivobulin isethionate demonstrated significant antitumor activity in a broad spectrum of murine and human tumor models that were cross-resistant to vincristine, cisplatin, vinblastine, navelbine, and doxorubicin and in tumor cell lines exhibiting multidrug resistance owing to P-glycoprotein overexpression. In animal studies, the activity of Mivobulin isethionate was largely independent of the route of drug administration but favored a prolonged treatment schedule. Unfortunately, in clinical trials, Mivobulin fail to demonstrate the significant activity
Status:
Investigational
Source:
INN:metrazifone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Metrazifone was developed as an analgesic agent. However, this drug has never been marketed.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bisnafide (previously known as DMP 840), a bis-naphthalimide derivative that was developed by Bristol-Myers Squibb as a potential anticancer agent. Bisnafide acts as DNA intercalator and topo II inhibitor. This drug participated in phase I clinical trials in pediatric patients with refractory solid tumors. However, further, development has been discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Lorapride is a centrally acting sulfonamide. It has pharmacodynamic properties that are mainly related to ulcer treatment. On the basis of its psychopharmacologic profile, it has no neuroleptic potential, but it does exhibit some psychostimulating components. After oral administration, absorption of lorapride was rapid. The rate of absorption was first order for solution and zero order for capsule.
Status:
Investigational
Source:
NCT01355497: Phase 3 Interventional Completed Muscle Wasting
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
MK-2866 (Gtx-024) is a selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting and osteoporosis. It is a non-steroidal agent with anabolic activity designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Bederocin (REP8839) is a novel methionyl-tRNA synthetase (MetS) inhibitor being developed by Replidyne (GlaxoSmithKline licensed REP8839 to Replidyne it). The biochemical activity of REP8839 was shown by specific inhibition of purified S. aureus MetS (50% inhibitory concentration, <1.9 nM). Target specificity was confirmed by overexpression of the metS gene in S. aureus, resulting in an eightfold increase in the MIC for REP8839. Macromolecular synthesis assays in the presence of REP8839 demonstrated a dose-dependent inhibition of protein synthesis and RNA synthesis in S. pneumoniae R6, but only protein synthesis was affected in an isogenic rel mutant deficient in the stringent response. REP8839 is a novel diary diamine-containing MetS inhibitor that has not been previously disclosed but is related to the previously described compounds and is currently being evaluated as a topical antibiotic for the treatment of skin infections and eradication of S. aureus from the anterior nares.
Class (Stereo):
CHEMICAL (RACEMIC)
Ronipamil was developed as a verapamil analogue with a longer duration of action. However, it has much less calcium antagonist action than verapamil. Ronipamil has been tested for its ability to reduce ischaemia-induced arrhythmias in conscious rats. Compared to similar compounds, ronipamil was less effective and produced no statistically significant antiarrhythmic effects in rats. It had limited haemodynamic effects and no marked actions on blood pressure and heart rate. In another study, ronipamil prolonged survival time after traumatic shock and was shown to possess anti-shock potential. No information on current development of this drug is available.
Status:
Investigational
Source:
NCT00664378: Phase 2 Interventional Terminated Relapsed and Refractory Multiple Myeloma
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
CYT997 (Lexibulin) is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. CYT997 (Lexibulin) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. CYT997 (Lexibulin) blocks the cell cycle at the G(2)-M boundary, and Western blot analysis indicates an increase in phosphorylated Bcl-2, along with increased expression of cyclin B1. Caspase-3 activation is also observed in cells treated with CYT997 (Lexibulin) along with the generation of poly(ADP-ribose) polymerase. The compound possesses favorable pharmacokinetic properties, is orally bioavailable, and is efficacious per os in a range of in vivo cancer models, including some refractory to paclitaxel treatment. CYT997 (Lexibulin) exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 (Lexibulin) possesses a useful combination of pharmacologic and pharmacokinetic properties having considerable potential as a novel anticancer agent. Lexibulin was being developed by YM BioSciences as a vascular-disrupting agent (VDA) for the potential treatment of cancer, it was in phase II development on YM BioSciences ' pipeline. It appears that the development of lexibulin has been discontinued.
