anti-neoplastic agent

Anti-Influenza agent 4 is a potent and selective inhibitor of the influenza virus, effectively inhibiting the A Parma and A Roma strains with EC50s of 62 nM and 150 nM, respectively.

Anti-TB agent 1 is a potent and orally active anti-tuberculosis compound (MICs: < 2 nM against the Mtb strains H37Rv, rRMP, and rINH).

Anti-inflammatory agent 49 is a potent inhibitor of Drp1-Fis1 interaction, inhibits GTPase, and can be used in the study of diseases caused by mitochondrial dysfunction.

Anti-inflammatory agent 34 shows moderate acute anti-inflammatory activity and analgesic activity in vivo.

Anti-MRSA agent 3 inhibits methicillin-resistant Staphylococcus aureus (MRSA) activity significantly (MIC: 0.098 μg/ml) with low toxicity to normal cells. anti-MRSA agent 3 has a high binding affinity for bacterial genomic DNA and a strong ability to disrupt bacterial cell walls and membranes.

Anti-Aβ agent 1A is a potent anti-amyloid-β agent. Anti-Aβ agent 1A significantly inhibits LPS-induced IL-1β, IL-6 and TNF-α levels and reduces H2O2-induced apoptosis in SH-SY5Y cells using the mitochondrial pathway, exhibiting antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used to study Alzheimer's disease.

Anti-TSWV agent 1 is a highly effective inactivator (EC50:144 μg/mL) of tomato spotted wilt virus (TSWV).

Anti-osteoporosis agent-1 (comp 4aa) is a potent RPA (replication protein A) inhibitor with an IC50 value of 18 μM [1].

Anti-amyloid agent-1 is a potent compound that inhibits amyloid aggregation, offering a promising approach for research into the treatment of amyloidosis [1].

Anti-inflammatory agent 52 (compound 7c) is an orally active, selective COX-2 inhibitor with demonstrated anti-HT29 metastatic activity, causing periodic arrest in the S phase and G2 M phase. This agent exhibits moderate anti-inflammatory efficacy alongside a notable safety profile. Additionally, it possesses the uncommon capability of inhibiting tumor development in a mouse model, indicative of anti-cancer properties [1].

Compound 2v (Anti-inflammatory agent 45) demonstrates anticancer properties with direct inhibitory impacts on the proliferation of various blood malignancies, such as leukemia, lymphoma, and myeloma cell lines. It induces apoptosis and suppresses nitric oxide production in HL60 leukemia cells (IC50 = 14.7 μM) [1].

Anti-inflammatory agent 8 (compound 13), designated as an anti-inflammatory agent 8, displays enhanced activity on the COX-2 enzyme compared to COX-1, with an IC50 value of 0.09 nM, and exhibits oral bioavailability [1].

Anti-Trypanosoma cruzi agent-1 (Compd E5) demonstrates a potent anti-Toxoplasma effect.

Anti-neurodegeneration agent 1, a neurodegeneration-targeting agent.

Anti-inflammatory agent 22 (compound 14a) is a potent orally active compound with anti-inflammatory properties, effectively inhibiting LPS-induced TNF-α production with an IC50 of 14.6 μM. Additionally, Anti-inflammatory agent 22 prevents adipogenesis and effectively suppresses limb lymphedema volume in mice, holding promise for treating inflammation-related conditions, particularly lymphedematous tissue disorders [1].

Anti-Trypanosoma cruzi Agent-4 is a Trypanosoma cruzi inhibitor utilized for the investigation of infections caused by this parasite.

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].

Anti-MRSA agent 7 (Compound 12) is a potent antibacterial compound that effectively inhibits S. aureus and E. coli DNA gyrases, as well as topo IV enzymes from the same organisms, with IC50 values of 0.185 μM, 0.365 μM, 0.341 μM, and 0.059 μM, respectively [1].

Anti-MRSA agent 2 (compound 14) is a potent inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg ml), exhibiting relatively low toxicity to normal cells. It strongly disrupts bacterial membranes and effectively binds to bacterial genomic DNA.

Anti-MRSA agent 1 is an MRSA inhibitor with an MIC value of 0.5 μg/mL and is effective in alleviating the effects of MRSA resistance.

Anti-melanoma agent 1 (Compound 5m) is an apoptotic inducer in melanoma cells.

Anti-inflammatory agent 62 mitigates acetaminophen-induced hepatotoxicity in HepG2 cells by modulating inflammatory and oxidative stress pathways [1].

Compound 13, also known as Anti-inflammatory agent 57 and classified as a pyranocoumarin, is a natural product extracted from the roots of Peucedanum praeruptorum. This compound possesses both multidrug-resistance (MDR) reversal properties and anti-inflammatory effects [1].

Compound 29 (Compound 7) is an anti-inflammatory agent that exhibits hepatoprotective activity [1].

Compound 5b (Anti-inflammatory agent 61) is a potent anti-inflammatory agent that diminishes TNF-α expression in LPS-induced inflammation within RAW 264.7 cells and mitigates APAP-induced inflammation in HepG2 cells [1].

Anti-TNBC agent-3 (compound 3g) is a compound that induces apoptosis and possesses anti-cancer cell proliferation properties. It effectively inhibits tumor growth and metastasis in xenograft models of triple-negative breast cancer (TNBC) [1].

Anti-inflammatory agent 56 (Compound 9), a selective COX-2 inhibitor with an IC50 of 0.54 μM, exhibits antioxidant and anti-inflammatory properties by inhibiting oxidative stress-induced cell death and neuroinflammation through the suppression of Keap1, COX-2, and iNOS. It demonstrates low acute toxicity in mice with an LD50 of 1000 mg kg [1].

Anti-inflammatory agent 23 is an anti-inflammatory agent that inhibits LPS-activated NO production (IC50: 0.449 μM). anti-inflammatory agent 23 exhibits good affinity for p65 protein.

Anti-inflammatory agent 38 (compound 23d) is a potent Nrf2/HO-1 pathway inhibitor, with an IC 50 value of 0.38 μM for NO . Nrf2/HO-1-IN-1 can significantly reduce the level of ROS in cells. Nrf2/HO-1-IN-1 can be used for researching anti-inflammatory [1] .

Anti-MRSA agent is a potent antagonist of MRSA (MIC50: 0.38 μg/mL) with low hERG activity (IC50: 40 μM). anti-MRSA agent also has low toxicity to mammalian cells and little potential to acquire bacterial resistance.

Anti-infective agent 1 (compound 3a) serves as a potent and selective antiprotozoal and antimycobacterial compound, demonstrating antiparasitic efficacy against P. falciparum and T. brucei rhodesiense with IC50 values of 10.95 and 0.06 μM, respectively, and displaying antimycobacterial properties against Mycobacterium smegmatis with a minimum inhibitory concentration (MIC) of 8 μg mL [1].

Anti-Influenza agent 3 (compound 11h) is a potent anti-influenza agent with low cytotoxicity for MDCK epithelial cells, inhibiting the M2 WT and S31N ion channel conductivity. It has an EC50 value of 3.29 μM for A HK 68 (H3N2, M2-WT) and 2.45 μM for A WSN 33 (H1N1, M2-S31N) strain [1].

Anti-inflammatory agent 65 (compound 29), a Hederagonic acid derivative, exhibits potent activity by inhibiting nitric oxide (NO) release, nuclear translocation of IRF3 and p65, and disrupting the STING IRF3 NF-κB signaling pathway, thus attenuating the inflammatory response [1].

Anti-inflammatory agent 58 exhibits IL-1β inhibition with an IC50 value of 1.08 μM and suppresses pro-inflammatory gene expression, protein secretion, and NF-κB phosphorylation [1].

Compound 43, also known as compound 3, is a 6-methoxyflavonol glycoside exhibiting anti-inflammatory activity. This agent, along with compound 44, is extractable from the aerial parts of Tetragonia tetragonoides [1].

Compound 133, also known as Anti-osteoporosis agent-7, is a potential anti-osteoporosis agent that exhibits significant inhibition of osteoclast formation.

Anti-virus agent 1 (compound 4i), a phosphoramidate prodrug of GS-5734, exhibits potent antiviral efficacy and is primarily utilized in coronavirus and Ebola virus (EBOV) research.

Anti-inflammatory agent 6 exhibits anti-inflammatory potential by blocking the phosphorylation of Iκb kinase α/β (IKKα/β), IκBα and nuclear factor kB p65 (NF-κb p65), which are key controllers of inflammation.

Anti-Trypanosoma cruzi agent-3 is an antiprotozoal agent.

Anti-infective agent 4 (compound 73) is an orally active Trypanosoma cruzi inhibitor with an IC50 of 0.016 μM. It effectively reduces parasite burden in vivo and is useful for studying infections.

Anti-NASH Agent 1 (Compound 3d), derived from Elafibranor, serves as a strong PPAR-α/δ agonist aimed at treating nonalcoholic steatohepatitis (NASH). At dosages of 3-10 mg/kg over four weeks, this compound ameliorates hyperlipidemia, liver fat degeneration, and inflammation in a methionine-choline deficiency (MCD)-induced NASH mouse model, exhibiting minimal hepatotoxicity while providing substantial hepatic protection [1].

Flo8, an anti-inflammatory and antioxidant agent, effectively suppresses the release of reactive oxygen species (ROS) and nitric oxide (NO) while inhibiting neuronal apoptosis by modulating inflammatory and apoptotic signaling pathways, showcasing potential utility in Parkinson's Disease (PD) research [1].

Anti-MRSA Agent 8 (Compound 7g), a derivative of DAPG, exhibits potent antibacterial properties by interacting with bacterial cell membranes and is useful for studying methicillin-resistant Staphylococcus aureus (MRSA) [1].

Anti-inflammatory agent 17 an orally active anti-inflammatory agent, demonstrates potent efficacy in inhibiting the release of IL-6 and TNF-α without causing cytotoxicity in in vitro experiments. Furthermore, in vivo studies confirm its anti-inflammatory activity. Given its attributes, Compound 17 holds promise for investigating Acute lung injury (ALI) [1].

Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial agent used in tuberculosis (TB) research, inhibiting the growth of Mtb H37Rv and M299 with MIC50 values of 2.3 and 7.8 μM, respectively. This compound also suppresses the expression of iNOS, thereby inhibiting NO, TNF-α, and IL-1β production [1].

Anti-Heart Failure Agent 1 is an orally available compound suitable for treating heart failure without causing vomiting, nausea, or restlessness.

Anti-inflammatory agent 1 is a chemical compound designated for reducing inflammation, structurally characterized by a [carboxyl acid], [oxygen], and [hydrocarbon] ring, with notable efficacy in mitigating inflammatory responses.

Anti-hyperglycemic agent 1 is a potent inhibitor of alpha-glucosidase (IC50: 0.53 μM). anti-Hyperglycemic agent 1 can be used to study diabetes.

Anti-parasitic agent 3 is effective against drug-resistant parasites.