antitumoral

Datelliptium chloride hydrochloride is a DNA-intercalating agent derived from ellipticine, exhibiting anti-tumor activities.

BI-1347 is a potent, selective inhibitor of CDK8/cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.

Antitumor agent-87 is a potent compound exhibiting high antitumoral activity, with a Ki value of 0.23 µM for CYP1A1. It demonstrates antiproliferative effects and induces cell cycle arrest at the G2/M phase, underscoring its effectiveness as an antitumor agent.

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

HDAC-IN-4, a selective HDAC6 and HDAC10 inhibitor (pIC50s: 7.2 and 6.8 in the BRET assay), exhibits antitumoral activity.

M8891 is an orally active, reversible, and brain-penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor (IC50: 54 nM; Ki: 4.33 nM). It inhibits the growth of primary endothelial cells and tumor cells, demonstrating both antiangiogenic and antitumoral activity.

JBJ-08-178-01, a mutant-selective tyrosine kinase inhibitor, targets (HER2) human epidermal growth factor receptor 2 and exhibits antitumoral activity. This compound not only diminishes HER2's kinase activity and protein levels through the induction of proteasomal degradation of the receptor but also shows promise in non-small-cell lung cancer research.

Decamethylene glycol is a substance used as a reagent in the biological study of modified oligonucleotide with in vivo antitumoral activity. Also used in the pharmaceutical study on the composition of essential oils obtained from myrrh and frankincense an

Bikaverin is a reddish pigment produced by different fungal species with antibiotic properties against certain protozoa and fungi. Bikaverin also has antitumoral activity against different cancer cell lines.

Antitumor agent-23 exhibits potent antitumoral activity, as demonstrated by its GI50 values of 38, 48, 5, 27, 80, and 28 nM against the lymphoma cell lines GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI respectively.

Norbatzelladine L, an inhibitor of both the catalytic and functional activities of the Pdr5p transporter, suppresses Pdr5p ATPase activity with an IC50 of 3.8 µM. Additionally, it exhibits antifungal, antiparasitic, antiviral, antibacterial, and antitumoral properties.

Batzelladine D, also known as Compound 1, functions as an inhibitor of the Pdr5p transporter's catalytic and functional activities, demonstrating inhibitory action against Pdr5p ATPase activity with an IC50 value of 7.1 µM. Additionally, it exhibits a range of bioactivities including antifungal, antiparasitic, antiviral, antibacterial, and antitumoral properties [1].

Stem bromelain (EC 3.4.22.32), a cysteine proteinase from pineapple (Ananas comosus) stem, is a significant type of bromelain known for its fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory properties. It also demonstrates in vivo antitumoral, antileukemic, and antimetastatic activities [1] [2].

Alloferon 2, an antiviral and antitumoral peptide, can be isolated from the hemolymph of the blow fly Calliphora vicina (Diptera) [1].

Alloferon 1 is a peptide with both antiviral and antitumor activities. It is capable of stimulating natural cytotoxicity of human peripheral blood lymphocytes, inducing the synthesis of interferon (IFN), and enhancing host resistance against viruses and tumors in mouse models. Additionally, Alloferon 1 exhibits anti-inflammatory effects in a λ-carrageenan-induced paw edema model. Alloferon 1 can be isolated from the blood of the dipteran blowfly Calliphora vicina.

Debio-0123 (WEE1-IN-5) is a potent, orally available and highly specific WEE1 inhibitor with an IC 50 in the low nanomolar range. Debio-0123 inhibits phospho-CDC2 which translated into an increase in DNA damage and premature entry into mitosis. Debio-0123 increases the antitumoral activity of Carboplatin in vivo whereas neither agent was active alone [1].