t 16

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

Antitrypanosomal agent 16 functions as a potent trypanocide, exhibiting an inhibitory concentration 50 (IC50) of 0.04μM against the T. congolense strain IL3000 [1].

Insecticidal agent 16 (compound A21) exhibits insecticidal activity against Plutella xylostella, with LC50 values of 1.2 and 13.2 µg mL respectively.

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

GLP-1 receptoragonist 16 (Example 53) is a GLP-1 agonist applicable for research in diabetes, obesity, or diseases related to non-alcoholic steatohepatitis.

Anti-inflammatory agent 16 (compound 14) is a potent peptidomimetic that significantly reduces the expression levels of TNFα, NO, CD40, and CD86 [1].

Antifungal agent 16 has antimicrobial activity comparable to that of ciprofloxacin and has higher antifungal activity than fluconazole.

Antimalarial agent 16 is a parasite inhibitor that exhibits antimalarial effects and inhibits the growth of Plasmodium falciparum with an IC50 value of 2.0 nM.

Anticancer agent 16 showed good cytotoxic effects on HCT-116 cell line (IC50: 8.55 μM), NCI-H460 cell line (IC50: 5.41 μM) and SKOV3 cell line (IC50: 6.4 μM).

Compound 115a, a GLP-1R agonist, effectively activates the GLP-1 receptor with an EC50 of 0.15 nM [1].

Maltodextrin (dextrose equivalent 16.5-19.5) serves as an excipient in pharmaceutical applications. Excipients, also known as pharmaceutical auxiliaries, are chemical substances utilized in drug formulation alongside active pharmaceutical ingredients. They primarily enhance the stability, solubility, and processability of drug preparations, while also influencing the absorption, distribution, metabolism, and elimination (ADME) of co-administered drugs [1].

CML-IN-1, also known as compound 7 and compound 4, is a potent anticancer agent that demonstrates a strong induced-apoptosis effect in the human chronic myeloid leukemia (CML) cell line K562. It diminishes protein phosphorylation within the PI3K Akt signaling pathway to exert its effects and suppresses cell proliferation through the inhibition of the MEK ERK signaling pathway in colorectal cancer [1] [2].

TLR7 agonist 16 (compound 16d) is a potent activator of TLR7 with an EC50 value of 18 nM, effectively triggering the activation of mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low-nanomolar levels [1].

Compound D16 (Anticancer agent 168) is an inhibitor of DNA2 that induces apoptosis and cell-cycle arrest predominantly in the S-phase. It demonstrates anticancer efficacy and can counteract chemotherapy resistance in cancers harboring mutant p53 [1].

Compound 166, also referred to as compound 3, exhibits potent anticancer properties, demonstrating significant inhibitory activity against Caco-2 cells with an IC50 value of 9.6 nM [1].

Anticancer agent 162 (compound 1d) is a potent theranostic agent that selectively induces oncosis in Hela cells, exhibiting pronounced lipophilicity and cytotoxicity [1].

Compound 3b, known as Anticancer Agent 161, is a bioactive alkynol exhibiting potential anticancer properties. It has the capability to induce autophagy and deplete mitochondrial membrane potential [1].

Anticancer agent 160 (Compound 6), a natural product extracted from Parthenium hysterophorus, exhibits cytotoxicity against HCT-116 cells with an IC50 of 5.0 μM [1].

Antibacterial agent 165 (compound 3), a hydroxyquinoline derivative, effectively inhibits methicillin-resistant Staphylococcus aureus (MRSA) [1], demonstrating potent antibacterial properties.

Antibacterial agent 163 (compound 1), a hydroxyquinoline derivative, potently inhibits methicillin-resistant Staphylococcus aureus (MRSA) [1].

Antibacterial agent 162 trifluoromethanesulfonate (compound 7), a dual-function molecule, demonstrates potent inhibitory effects on Staphylococcus aureus, including MRSA strains, and exhibits antiproliferative activity against colon cancer and non-small cell lung cancer cells. This compound is applicable in both anticancer and antibacterial research [1].

Compound 6 (Antibacterial agent 161, trifluoromethanesulfonate) exhibits antibacterial properties and demonstrates significant antiproliferative effects against colon cancer and non-small cell lung cancer [1].

Antibacterial Agent 160 is a potent antibacterial agent that rapidly eradicates bacteria and inhibits the formation of bacterial biofilms. It disrupts the normal functioning of DNA, resulting in cellular death [1].

Compound 167 (Antibacterial agent 167), identified as an inhibitor of pathogenic bacterial carbonic anhydrases, effectively inhibits the growth of N. gonorrhea strains. The inhibition occurs at concentrations between 16 to 64 µg mL [1].