nor 1

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

Ganciclovir sodium (Cytovene IV sodium) is the sodium salt of Ganciclovir with antiviral activity, especially against cytomegalovirus (CMV) and herpes simplex virus type 1 (HSV-1).

11-Oxomogroside IIa is a cucurbitane glycoside extracted from the fruits of Siraitia grosVenorii. It has inhibitory effects against the EBV-EA activation induced by TPA, shows weak inhibitory effects on activation of NOR 1, a nitric oxide (NO) donor.

(E Z)-Droloxifene is a mixture comprising (E)-Droloxifene, known as a selective estrogen receptor modulator, and (Z)-Droloxifene. (E)-Droloxifene binds to estrogen receptors (ER) in rabbit uterine homogenate with an IC50 of 24 nM. It increases uterine weight in immature rats and reduces the uterine weight increase caused by estradiol in juvenile rats. Additionally, (E)-Droloxifene inhibits the growth of human breast cancer cells MCF-7, ZR-75-1, and T47D stimulated by 17β-estradiol. In contrast, (Z)-Droloxifene shows weak binding to ER and exhibits neither estrogenic nor anti-estrogenic activity.

2-Bromo-1-decanal was synthesized as an affinity labeling probe for the aliphatic aldehyde site of Vibrio harveyi luciferase. In the presence of excess amounts of this probe, the inactivation of bacterial luciferase occurred following apparent first order

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

Phosphoramide mustard cyclohexanamine is the active metabolite of cyclophosphamide, an alkylating agent that cross-links DNA strands, organizes cell division and causes cell death, and has antitumor activity.

Norhyodeoxycholic acid (NHDCA) is a synthetic bile acid and a derivative of hyodeoxycholic acid .1,2 NHDCA is an intermediate in the synthesis of 3β-sulfooxy-7β-hydroxy-24-nor-5-cholen-23-oic acid, which has been used as an internal standard for the quantification of δ5-bile acid conjugates that have been identified in patients with Niemann-Pick disease type C1.3 |1. Schteingart, C.D., and Hofmann, A.F. Synthesis of 24-nor-5β-cholan-23-oic acid derivatives: A convenient and efficient one-carbon degradation of the side chain of natural bile acids. J. Lipid Res. 29(10), 1387-1395 (1988).|2. Une, M., and Hoshita, T. Natural occurrence and chemical synthesis of bile alcohols, higher bile acids, and short side chain bile acids. Hiroshima J. Med. Sci. 43(2), 37-67 (1994).|3. Kakiyama, G., Muto, A., Shimada, M., et al. Chemical synthesis of 3β-sulfooxy-7β-hydroxy-24-nor-5-cholenoic acid: An internal standard for mass spectrometric analysis of the abnormal δ5-bile acids occurring in Niemann-Pick disease. Steroids 74(9), 766-772 (2009).

1. Acetylshikonin exhibits weak cytotoxicity against human umbilical vein endothelial cells (HUVECs) with IC5 of over 2 microM, exhibits the antiangiogenic and antitumorigenic effects by suppressing proliferation and angiogenic factors. 2. Acetylshikonin inhibits the generation of NADPH oxidase complex in the activation of respiratory burst of PMNs, but does not directly inhibit the activity of NADPH oxidase already generated. 3. Certain shikonin derivatives(such as Acetylshikonin) act as modulators of the Nur77-mediated apoptotic pathway and identify a new shikonin-based lead that targets Nur77 for apoptosis induction. 4. Acetylshikonin, shikonin, and alkannin have accelerative effect on the proliferation of granulation tissue in rats. 5. Acetylshikonin has inhibitory effect on the edematous response is due neither to the release of steroid hormones from the adrenal gland nor to the glucocorticoid activity, but probably partly to the suppression of mast cell degranulation and partly to protection of the vasculature from mediator challenge. 6. Acetylshikonin induces apoptosis of hepatitis B virus X protein-expressing human hepatocellular carcinoma cells via endoplasmic reticulum stress.

β-Nor-lapachone is an antibiofilm agent of Candida glabrata with antifungal activity [1]. It stimulates ROS production, inhibits efflux activity, adhesion, biofilm formation, and disrupts the metabolism of mature biofilms.

Almurtide (nor-MDP), a derivative of muramyl dipeptide, exhibits anti-inflammatory and anti-tumor properties. It demonstrates protective effects in mice against infections caused by Pseudomonas aeruginosa when administered intraperitoneally and Candida albicans when administered intravenously. Furthermore, Almurtide has been shown to inhibit the carcinogenic Friend leukemia virus [1] [2] [3].

Anti-MRSA agent 4 (compound 7a), a selective and potent inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA) growth, demonstrates a minimum inhibitory concentration (MIC) of ≤ 0.26 µM and exhibits neither cytotoxic nor hemolytic activity in HEK293 cells [1].

Efflux pump-IN-2 is an AcrB efflux pump inhibitor that potentiates the effect of antibiotics and inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-2 does not disrupt the bacterial outer membrane nor display toxicity in a nematode model [1].

11-Oxomogroside II A1 (compound 7), an oxidized cucurbitin derived from the ethanol extract of Rohanberry fruit, inhibits the activation of Epstein-Barr virus (EBV) early antigen (EBV-EA) induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) and modestly inhibits the activation of (±)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor [1].

PZ-1922 (Compound 16), able to cross the blood-brain barrier, is a dual antagonist for 5-HT6R and 5-HT3R with K i values of 17 nM and 0.45 nM, respectively. It also reversibly inhibits MAO-B with a pIC50 of 8.93. Moreover, PZ-1922 mitigates scopolamine (SCOP)-induced memory deficits in rats as observed in the novel object recognition (NOR) test and hinders Aβ-induced memory impairment in the T-maze test [1].

Antiproliferative Agent-38 (COM 18), a tetracyclic compound, features a reactive ring nitrogen (likely the quinoline moiety) that resists N-alkylation. Despite its classification, it neither exhibits anti-malarial properties nor inhibits cancer cell proliferation [1].

23-Nor-6-oxopristimerol is a dinor-triterpene characterized by its phenolic structure [1].

Compound 9, 15-Nor-14-oxolabda-8(17),12E-diene-18-oic acid, is an isolated compound derived from the roots of Chloranthus spicatus [1].

(4S)-10-Nor-calamenen-10-one (Compound 15), an eudesmane sesquiterpene from Alpinia oxyphylla [1], enhances LPS-induced nitric oxide (NO) production in microglial cells.

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.

1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine (DAPE), a type of phospholipid phosphatidylethanolamine, does not markedly impact protein phosphatase PP2A activity nor does it inhibit the insulin-stimulated translocation of GLUT4 [1].

Mogroside III-A2 exhibits inhibitory effects with IC50 values of 346-400 mol ratio 32 pmol TPA. and shows weak inhibitory effects on activation of (+ -)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor.

(24xi)-24,25-Dihydroxycycloartan-3-one exhibits inhibitory effects on both EBV-EA and NOR 1 activation.

(24R)-Cycloart-25-ene-3beta,24-diol may be an anti-tumor promoter, it exhibits inhibitory effects on both Epstein-Barr virus early antigen (EBV-EA) and (+ -)-(E)-methtyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3- hexemide (NOR 1) activation.