MedChem Express
Antibacterial agent 198 (Compound 16) is an antibacterial agent against gram positive Staphylococcus aureus and strains of Entercoccus[1].
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Antibacterial agent 199 (Compound 2) is an activator for caseinolytic protease (ClpP) with a Kd of 0.7 μM. Antibacterial agent 199 exhibits antibacterial efficacy against Gram-positive strains Staphylococcus aureus, Streptococcus pneumoniae and Gram-negative strain Neisseria meningitidis, with MICs of 16, 0.5 and 0.5 μg/mL, respectively[1].
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Antibacterial agent 200 (pyridyl HH 7), a unique hydrazyl hydroxycoumarin (HH), has strong antibacterial efficacy and broad antibacterial spectrum with MIC values ranging from 0.5 to 32 μg/mL for Gram-positive and Gram-negative bacteria. Antibacterial agent 200 exhibits a good inhibition against Pseudomonas aeruginosa 27853 with a low MIC value of 0.5 μg/mL. Antibacterial agent 200 […]
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Antibacterial agent 201 (Compound 3) is an antibacterial agent through disruption of membrane integrity. Antibacterial agent 201 inhibits proliferation of Staphylococcus aureus strain RN4220, methacillin-resistane S. aureus, Pseudomonas aeruginosa strain PA01 and Escherichia coli strain ANS1 with MIC99s of 2.0, 1, 8.1 and 2.2 μg/mL, respectively[1].
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Antibacterial agent 202 (compound 45c) is a low cytotoxic bacterial inhibitor with good activity against Gram-negative bacteria, including Escherichia coli, Klebsiella pneumonia, especially Pseudomonas aeruginosa, (MIC (minimum inhibitory concentration)=7.8-31.25 μM). Antibacterial agent 202 can exert antibacterial activity by destroying the integrity of cell membranes and can be used in the research of bacterial infections[1].
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Antibacterial agent 203 (Compound 5h) has antibacterial and antifungal activity. Antibacterial agent 203 has potent antifungal activity against C. albicans, with a MIC of 3.90 μg/mL. Antibacterial agent 203 has antimicrobial activity on healthy mouse fibroblast cells (L929), with an IC50 of 75.96 μM[1].
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Antibacterial agent 204 (Compd P2-56-3) possesses potentiated Rifampin (RIF) activity against Acinetobacter baumannii and Klebsiella pneumoniae. Antibacterial agent 204 (Compd P2-56-3) disrupts the outer membrane of A. baumannii. T[1].
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Antibacterial agent 205 (Compound 10d) is a indolylacryloyl-derived oxacins, which exhibits broad antibacterial spectrum with MIC of 0.25-0.5 μg/mL. Antibacterial agent 205 reduces the exopolysaccharide, eliminates the biofilm, and thus attenuates the drug resistance. Antibacterial agent 205 exhibits antibacterial activity through destory of membrane integrity, accumulation of reactive oxygen species ROS, and inhibition of DNA […]
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Antibacterial agent 206 (Compound 10e) is a indolylacryloyl-derived oxacins, which exhibits broad antibacterial spectrum with MIC of 0.25-1 μg/mL. Antibacterial agent 206 reduces the exopolysaccharide, eliminates the biofilm, and thus attenuates the drug resistance. Antibacterial agent 206 exhibits antibacterial activity through destory of membrane integrity, accumulation of reactive oxygen species ROS, and inhibition of DNA […]
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Antibacterial agent 207 (Compound Ru1) has antibacterial activity against S. aureus (MIC: 1 μg/mL), and low resistance frequencies. Antibacterial agent 207 destroys the bacterial cell membrane, promote production of ROS in bacteria[1].
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Antibacterial agent 210 (compound A9), an amide derivative, is a Pseudomonas aeruginosa quorum sensing inhibitor (QSI). Antibacterial agent 210 inhibits the quorum sensing systems by binding with LasR and PqsR, especially PqsR[1].
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Antibacterial agent 211 (compound k15) has bactericidal activity against clinically isolated MRSA and VRE (MICs = 0.25–1.00 μg/mL). Antibacterial agent 211 avoids resistance by damaging biofilm and targeting cell membranes[1].
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Antibacterial agent 212 (Compound 162) is an antibacterial agent with oral activity and good pharmacokinetic properties, having a MIC of 4 μg/mL against Pseudomonas aeruginosa T-2022-D2-048[1].
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Antibiofilm agent-5 (compound 6c) is a multitargeting antibacterial agent with potent antibiofilm activity. Antibiofilm agent-5 could induce metabolic dysfunction by deactivating lactate dehydrogenase and promote the accumulation of reactive oxygen species to decrease the reduced glutathione and ultimately cause oxidative damage in bacteria. Antibiofilm agent-5 can be used for the research of refractory biofilm-intensified bacterial […]
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Antibiofilm agent-6 (Compound 26c) is a quorum sensing inhibitor with strong antibiofilm effects that can inhibit the fluorescence intensity of PAO1-lasB-gfp and PAO1-pqsA-gfp in a concentration-dependent manner. Antibiofilm agent-6 can inhibit the production of pyocyanin and rhamnolipid. Antibiofilm agent-6 aids helps ciprofloxacin (HY-B0356) effectively eliminate the living bacteria in a mouse model infected with P. […]
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Antibody inhibitors are compounds with the same activity as the original therapeutic antibodies, which can be used as positive controls for drug efficacy evaluation and other studies. Antibody inhibitors can also assist in verifying the functional activity of the target protein. These antibody inhibitors are active in vivo and can achieve certain physiological functions by […]
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Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells[1].
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Anticancer agent 188 (compound D43) inhibits DNA synthesis in TNBC cells, leading to cell cycle arrest at the G2/M phase. Anticancer agent 188 has anti-cancer viability by inducing ROS-mediated apoptosis and DNA damage[1].
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MedChem Express
Anticancer agent 190 (compound 3e) is an inhibitor targeting KSP (Kinesin) and PI3Kδ with activity against breast cancer[1].
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Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research[1].
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Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test[1].
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Anticancer agent 193 (compound D3-3) is an inducer of ferritinophagy, eventually triggering ferroptosis. Anticancer agent 193 induces the production of lipid ROS, and significantly promoted colorectal cancer cells to release the ferrous ion in an autophagy-dependent manner[1].
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Anticancer agent 194 (compound 10p) is a ferroptosis and autophagy inducer. Anticancer agent 194 arrests colon cancer cell cycle at G2/M phase, but can’t induce cell apoptosis. Anticancer agent 194 independently triggeres cell ferroptosis and autophagy through the massive accumulation of ROS[1].
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Anticancer agent 195 (Compound 10) is an inhibitor for ELF3-MED23 PPI with Ki of 0.68 μM. Anticancer agent 195 induces apoptosis and exhibits antitumor activity[1].
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Anticancer agent 196 (compound 1) shows cell cytotoxicity with IC50 values of 7.69 µM and 54.2 µM for HL-60 cells and A549 cells, respectively. Anticancer agent 196 can induce DNA damage[1].
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Anticancer agent 197 (compound 2b) shows cell cytotoxicity with IC50 values of 10.03 µM and 73.54 µM for HL-60 cells and A549 cells, respectively. Anticancer agent 197 can induce DNA damage[1].
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Anticancer agent 198 (compound 18b) is a potent anticancer agent and potential WRN protein inhibitor. Anticancer agent 198 was significantly toxic to K562 cells and WRN-overexpressing PC3 cells[1].
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Anticancer agent 199 (Compound G-4) induces apoptosis in triple negative breast cancer (TNBC) cells via the mitochondrial pathway through inhibiting EGFR, AKT and MAPK pathways. Anticancer agent 199 also induces Ferroptosis by down-regulating LCN2. Anticancer agent 199 inhibits TNBC cell viability and migration, and induces S phase cell cycle arrest. Anticancer agent 199 is a […]
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MedChem Express
Anticancer agent 201 (Compound 2f) has IC50 values in the low micromolar range for multiple tumor cell lines. Anticancer agent 201 is highly cytotoxic to CCRF-CEM cells in vitro, inducing apotosis by activating caspase-3 in the intrinsic mitochondrial pathway and lysis of PARP, as well as reducing the expression of Bcl-2 and Bcl-XL proteins. Anticancer […]
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Anticancer agent 203 (compound 27) is an anticancer agent. Anticancer agent 203 shows cytotoxicity. Anticancer agent 203 has the potential for the research of hepatoma[1].
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Anticancer agent 204 (Compound 6), a cinnamide fluorinated derivative, possesses anticancer activity. Anticancer agent 204 can arrest the cell cycle of HepG2 cells in the G1 phase and induce apoptosis by reducing the level of mitochondrial membrane polarization (MMP)[1].
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Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. […]
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Anticancer agent 207 (compound 10b) is a potent anticancer agent. Anticancer agent 207 bounds to the NRAS rG4 with a KD value of 2.31 µM. Anticancer agent 207 shows cytotoxicity and decreases the expression of NRAS protein. Anticancer agent 207 shows antitumor activity[1].
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Anticancer agent 210 (Compound 7a) is a Gefitinib (HY-50895) derivative. Anticancer agent 210 inhibits proliferation, migration and colony formation of cancer cells. Anticancer agent 210 induces apoptosis in cells H1299[1].
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Antidepressant agent 6 (S-3a) is a lead compound with potent and sustained antidepressant effects. Antidepressant agent 6 (S-3a) displays high cognitive safety margin.Antidepressant agent 6 (S-3a) antagonizes M1 receptors and elevates BDNF levels, suggesting its potential as an antidepressant for further exploration[1].
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Antidiabetic agent 5 (compound S1) is a antidiabetic agent. Antidiabetic agent 5 inhibits the activity of α-glucosidase and α-amylase with IC50 values of 3.91, 8.89 µM, respectively. Antidiabetic agent 5 decreases sugar levels. Antidiabetic agent 5 has the potential for the research of type-II diabetes[1].
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Antifungal agent 100 (compound 3i) has significant antifungal effects against S. sclerotiorum with an EC50 value of 0.33 mg/L. Antifungal agent 100 has an IC50 of 0.63 mg/mL against the Succinate dehydrogenase (SDH) of S. sclerotiorum[1].
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Antifungal agent 90 (Compound 7n) is an antifungal agent that inhibits ergosterol biosynthesis. Antifungal agent 90 showed excellent antifungal activity against Valsa mali and Botrytis cinerea with EC50 values respectively. 4.26 and 1.41 μg/mL[1].
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Antifungal agent 91(compound 1) is a dihydroflavonol that can be isolated from the leaves of Artocarpus elasticus. Antifungal agent 91 is a PTP1B inhibitor with an IC50 value of 0.17 μM. Antifungal agent 91 has antifungal activity[1].
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Antifungal agent 92 (Compound 21) is a potent antifungal agent with an EC50 of 4.4 μM against Sclerotinia sclerotiorum. Antifungal agent 92 can induce abnormal mitochondrial morphology, loss of mitochondrial membrane potential, and reactive oxygen species (ROS) accumulation in Sclerotinia sclerotiorum. Antifungal agent 92 is a moderate promiscuous inhibitor of mitochondrial complexes II and III[1].
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Antifungal agent 93 (compound 10) is a potent antifungal agent. Antifungal agent 93 shows antimicrobial activity[1].
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Antifungal agent 94 (Compound 49) is a Flavonoid derivative, which exhibits antifungal activity with EC50 of 0.28 μM and a half-maximal effective concentration of 0.46 μg/mL against Rhizoctonia solani[1].
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Antifungal agent 95 (Compound CN21b) is an antifungal agent for Sclerotinia sclerotiorum and Botrytis cinerea, with EC50s of 2.11 and 0.97 μM, respectively. Antifungal agent 95 exhibits antifungal activity against resistant B. cinerea strains, with EC50s less than 10 μM[1].
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Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively[1].
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Antileishmanial agent-26 (Compound 69) is a guanidine-containing compound with anti-Leishmania donovani activity. Its IC50 value against Leishmania donovani is 5.67 μM, and its CC50 value against THP-1 is 3.79 μM. Antileishmanial agent-26 can be used in the research of tropical diseases[1].
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Antileishmanial agent-27 (compound 7j) is a benzothiazolo-coumarin derivative. Antileishmanial agent-27 is a competitive inhibitor of arginyl-tRNA synthetases (ArgRSs). Antileishmanial agent-27 shows selectivity toward ArgRS of Leishmania donovani (LdArgRS) than its human counterpart (HsArgRS), with IC50 values of 1.2 and 19 μM, respectively. Antileishmanial agent-27 possesses high pharmacokinetic properties[1].
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