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

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Showing 841 - 850 of 4227 results

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

Class (Stereo):
CHEMICAL (ACHIRAL)



Tolimidone, Lyn protein-tyrosine kinase stimulant, is in phase II clinical by Melior Discovery and Bukwang for the treatment of type 2 diabetes. It is also in phase II clinical by Pfizer for the treatment of ulcer. However, this research has been discontinued.
Status:
Investigational
Source:
NCT04439188: Phase 2 Interventional Active, not recruiting Advanced Lymphoma
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GSK-2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK-2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. On April 1 2016 GlaxoSmithKine completes a phase-I/II trial for Solid tumours (Late-stage disease) in USA, United Kingdom and South Korea (NCT01458067).
Status:
Investigational
Source:
NCT03480971: Phase 2 Interventional Recruiting Mucositis
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tempol is used as an industrial catalyst and chemical oxidant. However, its ability to scavenge free oxygen species has generated interest in the biochemical potential of this compound. Biologically Tempol catalyzes the disproportionation of superoxides, facilitates hydrogen peroxide metabolism, and inhibits Fenton chemistry. These properties generated investigational interest for the use of tempol to mediate radiation damage during chemotherapy. Tempol has been used in human clinical trials for mitigation of radiation damage in related to anal cancer, and brain cancer. Tempol has also been investigated in a number of animal and invitro models for conditions, such as oxidative damage, brain hemorrhage, anxiety, malaria, platelet agregation,
Status:
Investigational
Source:
NCT02211872: Phase 1 Interventional Completed Neoplasms
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



BI-2536, an inhibitor of Polo-like kinase 1 (Plk-1) was being investigated by Boehringer Ingelheim as a possible treatment for cancer. BI-2536 inhibits Plk1 enzyme activity at low nanomolar concentrations. The compound potently causes a mitotic arrest and induces apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature. BI-2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens. In treated tumors, cells arrest in prometaphase, accumulate phosphohistone H3, and contain aberrant mitotic spindles. This mitotic arrest is followed by a surge in apoptosis, detectable by immunohistochemistry and noninvasive optical and magnetic resonance imaging. For addressing the therapeutic potential of Plk1 inhibition, BI-2536 has progressed into clinical studies in patients with locally advanced or metastatic cancers. It underwent phase II clinical studies for the treatment of breast cancer; non-small cell lung cancer; pancreatic cancer; prostate cancer; small cell lung cancer, but these studies were discontinued later.
Status:
Investigational
Source:
NCT01009931: Phase 2 Interventional Terminated Leukemia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phorbol 12-myristate 13-acetate (PMA) also commonly known as 12-O-Tetradecanoylphorbol-13-acetate (TPA) is a phorbol ester that is commonly used to activate phospholipid-dependent protein kinase (protein kinase C). PMA/ TPA possesses potential antineoplastic effects and was studied in phase II clinical trials together with dexamethasone in patients with relapsed or refractory acute myeloid leukemia. In addition, PMA/ TPA participated in phase I trial for treating patients with hematologic cancer or bone marrow disorder that has not responded to previous treatment. Nevertheless, both clinical trials were terminated. Besides, PMA/ TPA was studied in patients with solid tumors, which had depressed white blood cell and neutrophil counts because of prior treatment with cytotoxic cancer chemotherapeutic drugs. It was shown, that the drug increased the low white blood cell and neutrophil counts toward the normal range.
Status:
Investigational
Source:
Trans R Soc Trop Med Hyg. 1985;79(6):848-51.: Not Applicable Human clinical trial Completed Necatoriasis/blood/epidemiology
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Tetrachloroethylene is a nonflammable colorless liquid. Other names for tetrachloroethylene include perchloroethylene, PCE, PERC, tetrachloroethene, and perchlor. Tetrachloroethylene is used as a dry cleaning agent and metal degreasing solvent. It is also used as a starting material (building block) for making other chemicals and is used in some consumer products. It has also been used in water repellants, paint removers, printing inks, glues, sealants, polishes, and lubricants. Tetrachloroethylene has been in commercial use since the early 1900s. Tetrachlorethylene has been suspected of causing some types of cancer, based on both human and animal evidence. Laboratory studies have found that ingesting or inhaling tetrachlorethylene increased the risk of liver cancer in mice. In rats, inhaling tetrachloethylene was linked to kidney cancer and a rare type of leukemia. EPA has classified tetrachloroethylene as likely to be carcinogenic to humans by all routes of exposurebased on suggestive evidence in epidemiological studies and conclusive evidence in rats (mononuclear cellleukemia) and mice (increased incidence of liver tumors). The International Agency for Research on Cancer(IARC) has classified tetrachloroethylene as probably carcinogenic to humans (Group 2A).
Status:
Investigational
Source:
NCT02664181: Phase 2 Interventional Completed Lung Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Tetrahydrouridine is a potent competitive reversible inhibitor of cytidine deaminase. Tetrahydrouridine can inhibit cell proliferation by regulation of the cell cycle independent of cytidine deaminase (CDA) expression levels. Tetrahydrouridine may be useful for researching potential treatments for high CDA-expressing tumors. Tetrahydrouridine use, alone or in combination with the DNA methyltransferase inhibitor 5-fluoro-2’-deoxycytidine, is being evaluated in animal models and clinical trials for diseases, including cancer and mitochondrial DNA depletion syndrome.
Status:
Investigational
Source:
NCT00273884: Phase 2 Interventional Completed Acute Myeloid Leukemia
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amonafide L-malate (AS1413, Xanafide) is a DNA intercalator and topoisomerase II inhibitor that induces apoptosis by disrupting chromatin organisation independently of ATP. This is different from classical topoisomerase II inhibitors which induce apoptosis by causing extensive DNA damage. Amonafide L-malate is also able to evade P-glycoprotein and related transporters that contribute to multi-drug resistance. AS1413 had orphan drug status in both the U.S. and the E.U. for the treatment of AML and also received Fast Track status from the U.S. FDA for the treatment of secondary AML. Amonafide L-malate was originated by Xanthus Pharmaceuticals. It was added to Antisoma's pipeline through the acquisition of Xanthus Pharmaceuticals, Inc. in June 2008. Antisoma discontinued development of Amonafide L-malate after data from the open-label, international Phase III ACCEDE trial in over 420 patients showed that 600 mg/m 2 IV amonafide for 5 days plus cytarabine missed the primary endpoint of significantly improving initial remission rate, defined as the proportion of patients who achieve CR or CRi, vs. daunorubicin plus cytarabine.

Class (Stereo):
CHEMICAL (ACHIRAL)

1-(Phenylazo)-2-Naphthylamine (C.I. Food Yellow 10) is a synthetic lemon yellow azo dye primarily used as a food coloring