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Status:
Designated
Source:
EU-Orphan Drug:EU/3/13/1226
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Boldine, an aporphine alkaloid, found abundantly in the leaves/bark of boldo (Peumus boldus Molina) widely consumed in the folk medicine of some regions. Boldine possesses various pharmacological properties including, anticancer activity. It exhibits a significant improvement of learning and memory through inhibition of brain acetylcholinesterase activity and alleviation of brain oxidative stress, which was shown on animal models. Boldine is a potentially useful agent for the treatment of leishmaniosis. In addition, it suppresses osteoclastogenesis, improves bone destruction and may be a potential therapeutic agent for rheumatoid arthritis. Besides, was shown, that boldine inhibits telomerase in cells treated with sub-cytotoxic concentrations. Telomerase inhibition occurs via down-regulation of human telomerase reverse transcriptase (hTERT), the catalytic subunit of the enzyme.
Status:
Designated
Source:
FDA ORPHAN DRUG:10685
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Allopurinol riboside is a metabolite of allopurinol, a xanthine oxidase inhibitor indicated for the management of patients with leukemia, lymphoma, and solid tumor malignancies who are receiving cancer therapy which causes elevations of serum and urinary uric acid levels and who cannot tolerate oral therapy. Allopurinol riboside is not an inhibitor of xanthine oxidase. Allopurinol riboside is commonly thought to be directly synthesized by purine nucleoside phosphorylase (PNP) in vivo. Allopurinol riboside competitively inhibits the action of PNP on inosine in vitro. Allopurinol riboside potently inhibits growth in vitro of promastigotes of Leishmania species. Patients with American cutaneous leishmaniasis who received allopurinol riboside had clinical improvement. In addition, allopurinol riboside demonstrated some effectivity against Trypanosoma cruzi infections in animals.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Monastrol is a small, cell-permeable molecule that arrests cells in mitosis by specifically inhibiting Eg5, a member of the Kinesin-5 family. Monastrol has been used to probe the dynamic organization of the mitotic spindle. Monastrol inhibits both the basal and the microtubule-stimulated ATPase activity of the Eg5 motor domain. Unlike many ATPase inhibitors, monastrol does not compete with ATP binding to Eg5. Monastrol appears to inhibit microtubule-stimulated ADP release from Eg5 but does not compete with microtubule binding, suggesting that monastrol binds a novel allosteric site in the motor domain. (S)-monastrol, as compared to the (R)-enantiomer, is a more potent inhibitor of Eg5 activity in vitro and in vivo. As Monastrol, by specifically inhibiting kinesin Eg5, can cause mitotic arrest and monopolar spindle formation, it exhibits antitumor properties. Monastrol has being shown to be a potent inhibitor of pteridine reductase (PTR1) in Leishmania; it inhibits proliferation of amastigotes with an IC(50) (50% inhibitory concentration) of 10 uM in macrophage cultures infected with an L. donovani clinical isolate, with no host cytotoxicity. In experimental animals, oral administration of a 5 mg/kg dose of monastrol on two alternate days inhibits 50% of parasite growth, giving therapeutic backing to the use of monastrol as a potent antileishmanial in human VL cases.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Canthin-6-one is a natural product isolated from various plant genera and from fungi with potential antitumor activity. It induces cell death, cell cycle arrest and differentiation in human myeloid leukemia cells. Canthin-6-one is main compound isolated from Zanthoxylum chiloperone var angustifolium with broad spectrum antifungal, leishmanicidal and trypanocidal activities. Canthin-6-one exhibited trypanocidal activity in vivo in the mouse model of acute
or chronic infection. Canthin-6-one exhibited a broad spectrum of activities against Aspergillus fumigatus, A. niger, A. terreus, Candida albicans, C. tropicalis, C. glabrata, Cryptococcus neoformans, Geotrichum candidum, Saccharomyces cerevisiae, Trichosporon beigelii, Trichosporon cutaneum and Trichophyton mentagrophytes var. interdigitale with MICs values between 5.3 and 46 umol/L.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Angoroside C is a potential anti-inflammatory compound. Inhibitor of prostaglandin E2 release in mouse peritoneal macrophages in vitro. Shows potent antioxidative activity in reducing the oxidized OH adducts of dAMP and dGMP. Reveals some trypanocidal potential.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Palitantin is an antifungal and antiprotozoal compound used in biochemical research. Palitantin was first isolated as a metabolite of Penicillium
palitaus by Birkinshaw and Raistrick in 1936. Palitantin possess moderate antimycobacterial activity.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Harpagide and harpagoside are two iridoid glycosides existing in many medicinal plants. They are believed to be the main bioactive compounds related to the anti-inflammatory efficacy of these plants. In vitro Harpagide has shown cytotoxic activity against tumor cell lines A431, HeLa and MCF7. Harpagide emerged as a leishmanicidal agent. Harpagide is common in nature and is known to possess anti-inflammatory activity. In addition, it has been shown that the hydrolysed products of harpagoside and harpagide have more pronounced anti-inflammatory activity when compared to the unhydrolysed compounds.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Skimmianine is a newly discovered strong acetylcholinesterase (AChE) inhibitor, which can be used as promising candidate for L. braziliensis due to its potent immunomodulatory activity. In addition, because skimmianine has multi-targeted mechanism of action, it can be suggested for therapeutic efficacy in various inflammatory diseases.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Oryzalin is a selective preemergence surface-applied herbicide used for control of annual grasses and broadleaf weeds in fruit trees, nut trees, vineyards, established bermudagrass turf and established ornamentals. It inhibits the growth of germinating weed seeds. Oryzalin is an effective inhibitor of human
carbonic anhydrases (CAs). Eleven out of 12 catalytically active human CAs were strongly
inhibited by oryzalin and exhibited affinities of approximately 2–2000 nM. Oryzalin has been shown to bind specifically to plant tubulin in vitro, inhibited
its polymerization, and partly depolymerize taxol-stabilized
microtubules. It also inhibits polymerization of leishmania microtubules in vitro.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
P-nitroaniline is a chromogenic molecule that is used as a dyestuff intermediate in industrial applications. In biochemical research, enzyme assays utilize modified aminoacyl or peptidyl p-nitroanilines as substrates. The enzyme catalyzes the release of free p-nitroaniline, which is the basis of the colorimetric determination of the enzyme activity. Applications of the colorimetric properties of p-nitroanilide include the design of biopolymer drug delivery systems and of solid supports for enzyme immobilization. A kinetic analysis of the α-chymotrypsin catalyzed hydrolysis of aminoacyl and peptidyl p-nitroanilide substrates in vesicles has been reported. It has been shown to possess anti-leishmanial activity.