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

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Showing 391 - 400 of 4343 results

Status:
Investigational
Source:
INN:verubulin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Veribulin is a novel microtubule destabilizer that both functions as a potent cytotoxin and acts as a vascular disrupting agent (VDA). It binds to the same (or nearby) sites on β-tubulin as colchicine. It is capable of evading multidrug resistance pumps and, thus, achieves high CNS concentrations. It is efficacious in multiple xenograft models without CNS toxicity. Veribulin had previously demonstrated pre-clinical and clinical activity in multiple tumor types. Veribulin is in phase II clinical trial for the treatment of Glioblastoma and Malignant melanoma.
Status:
Investigational
Source:
INN:cethexonium chloride
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Cethexonium is a cyclohexanols derivative with antimicrobial activities.
Status:
Investigational
Source:
INN:tubulozole [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tubulozole is a stereospecific microtubule inhibitor. Structurally it is related to the benzimidazole carbamates by its carbamate moiety, which is essential for the activity of both types of compounds. The compound exists as a cis-isomer called tubulozole-C (R 46 846) and as a trans-isomer called tubulozole-T. The cis-isomer appears to be a potent and specific microtubule inhibitor, the trans-isomer being inactive at 100 times higher concentrations. At low concentrations, both isomers of tubulozole (C, T) inhibit Plasmodium falciparum but only tubulozole C inhibits mammalian cells. Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules. Tubulozole-C, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells. The activity of Tubulozole-C in experimental tumor systems can be explained partly by a direct antimitotic effect and partly by the disintegration of the normal subcellular organization of the nondividing cells. At concentrations which affect the microtubule system, tubulozole-C arrested directional migration of transformed cells and malignant invasion in a three-dimensional organ culture system. Investigations in vivo show that malignant L1210 leukemia cells are more susceptible to the antimicrotubular effect of tubulozole-C than are the normal leukocytes of the host. The trans-isomer of tubulozole (tubulozole-T, R 48 265), which has no antitumor activity in vivo, did not affect the microtubule system of cells in vitro or their capacity for directional migration or for malignant invasion.
Status:
Investigational
Source:
INN:semapimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.
Status:
Investigational
Source:
INN:fosdevirine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:iocanlidic acid (¹²³I) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Iocanlidic Acid I-123 is a radiolabeled phenylfatty acid derivative studied as a diagnostic agent for myocardial imaging
AZD8055 is a new ATP-competitive mTOR kinase inhibitor that was developed to overcome the limitations of the first generation of allosteric mTORC1 inhibitors (rapamycin and its analogs) as anticancer agents. AZD8055 potently and selectively inhibits mTOR by directly targeting its catalytic site, which results in the blockade of the activity of both mTORC1 and mTORC2 complexes. It displays antitumoral activity by inhibiting proliferation and/or inducing cell death in various cancer cell models, including ovarian clear cell carcinoma.
Status:
Investigational
Source:
INN:pomaglumetad methionil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

LY404039 [(-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid] is an agonist of orthosteric metabotropic glutamate receptor (mGluR)2/3. In addition, it acts as an agonist at dopamine D2 receptors. LY404039 demonstrated broad antipsychotic and anxiolytic efficacy across multiple animal models. LY-2140023 is a methionine amide prodrug of LY-404039 being developed by Eli Lilly & Co for the potential oral treatment of schizophrenia.
Status:
Investigational
Source:
NCT00655421: Phase 3 Interventional Unknown status Oral Cancer
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Toluidine Blue (also known as tolonium chloride or Toluidine blue O) is metachromatic dye used for a variety of histological staining, it selectively stains acidic tissue components (sulfates, carboxylates, and phosphate radicals. Toluidine blue has an affinity for nucleic acids, and therefore binds to nuclear material of tissues with a high DNA and RNA content. It was evaluated the toluidine blue staining in premalignancies, and superficial oral ulceration suggesting malignancy. The study showed 100% sensitivity in the detection of in situ and invasive carcinoma and no false-negative results occurred. The lesions that were diagnosed as dysplasia did not retain stain, and thus gave false-negative results. The reasons could be that the exact mechanisms by which the dye differentially stains malignant or dysplastic tissues remain unknown.
Status:
Investigational
Source:
NCT03189394: Phase 1 Interventional Unknown status HIV Infections
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fluridone, an herbicide that used for controlling invasive aquatic plants such as hydrilla in surface water bodies. It inhibits carotenoid synthesis in targeted plant species, preventing photosynthesis and ultimately causing mortality. This compound contains a 4(1H)-pyridone and a trifluoromethyl-benzene moiety, which are also present in molecules with analgesic and anti-inflammatory properties. Experiments on rodents have confirmed that fluridone could represent a new prototype of an anti-inflammatory drug.