antitrypanosomal

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor (IC50: 3.3 μM) that also inhibits glutathione reductase (IC50: 64.8 μM) and T. brucei (EC50: 1 μM).

Fexinidazole (HOE 239) is an antiparasitic agent with activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone.

Antitrypanosomal agent 2 shows potent and specific antiparasite activities against Trypanosoma brucei.

Compound C-1 (Antitrypanosomal agent 21) serves as an inhibitor of Trypanosoma brucei. It effectively reduces the levels of D6XM23 in the parasite lysate.

Antitrypanosomal agent 4 (compound 19) is a potent antitrypanosomal compound that crosses the blood-brain barrier and exhibits strong resistance to Trypanosoma cruzi and T. b. brucei with IC50 values of 1.2 μM and 70 nM, respectively.

The antitrypanosomal agent 8 (compound 3b) demonstrated a potent effect against Trypanosoma brucei with an IC50 of 0.79 μM, while the IC50 value was 80.95 μM.

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent demonstrating good ADME properties, with an IC50 of 0.47 μM against Trypanosoma brucei (T. brucei), making it more than twice as active as Nifurtimox; it also exhibits a strong interaction with and selective binding to AT-rich DNA.

The Antitrypanosomal agent 7 (compound 18c) is a potent anti-trypanosome agent and shows good ADME properties. The Antitrypanosomal agent 7 was more than two-fold more active against T. brucei (IC50: 0.71 μM) than Nifurtimox. Antitrypanosomal agent 7 has a strong interaction with DNA and can selectively bind to AT-rich DNA.

Antitrypanosomal agent 10, an antitrypanosomal compound, effectively inhibits Trypanosoma cruzi with an IC50 of 0.28 μM.

Antitrypanosomal Agent 11 is a chemical compound effective against Trypanosoma cruzi, exhibiting an inhibition concentration (IC 50) of 0.23 μM.

Antitrypanosomal agent 9 is a potent compound with inhibitory activity against T. b. brucei, exhibiting an IC50 of 1.15 μM. It is utilized in research for human African trypanosomiasis (HAT).

Antitrypanosomal agent 12, a C20-phenylthiourea, exhibits trypanocidal and cytotoxic activities, demonstrating antitrypanosomal activity with GI50 values of 0.22 μM. It induces faster cell swelling in bloodstream-form trypanosomes compared to Salinomycin [1].

Compound 4b (antitrypanosomal agent 13) is a potent antitrypanosomal with notable trypanocidal and cytotoxic activities, exhibiting GI50 values of 0.18 μM against T. brucei and 8.4 μM for HL-60 [1].

Antitrypanosomal agent 14 (Compound 1), a potent T. brucei inhibitor with an effective concentration (EC50) of 0.47 μM, also inhibits Tb GSK3 with an inhibitory concentration (IC50) of 12 μM, and is utilized in the research of Human African Trypanosomiasis [1].

Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1].

Compound 18 (compound 8b), a nitrofuran derivative, exhibits potent in vitro trypanocidal activity, with an IC50 value of 0.03 μM [1].

Compound 17 (Compd 7a) exhibits potent antiamastigote activity, demonstrated by its IC50 value of 0.03 μM against the T. congolense strain IL3000 [1].

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

Antitrypanosal agent 5 is a selective anti-trypanosomal agent that acts on T. brucei (IC50: 1 nM) and HEK293 cells (IC50: 483.3 μM).

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

Girinimbine (Girinimbin) is a carbazole alkaloid isolated from the plants M. koenigii, M. koenigii, and Murraya koenigii. Girinimbine exhibits a wide range of biological effects, including apoptosis, antitrypanosomal, antiplatelet, antimicrobial, anti-inflammatory, antioxidant, and antitumor activities.

Puromycin (NSC-3055) is an antibiotic protein synthesis inhibitor. It inhibits protein synthesis by binding to RNA. It also serves as an anticancer drug by suppressing the growth and metastasis in esophagus cancer cells by Akt phosphorylation. It is an antineoplastic and antitrypanosomal agent and is used in research as an inhibitor of protein synthesis.

SDZ285428 is a CYP24A1 inhibitor.