antileukemic

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

K00135 (IMIDAZOPYRIDAZIN 1) is a selective inhibitor of Pim kinases and can be used in studies about gastric cancer and antileukemic therapeutics.

Anticancer agent 110 is an anticancer compound with cytotoxic, antitumor, and antileukemic activity that triggers DNA damage and apoptosis and is used in the study of chronic granulocytic leukemia.

Coralyne chloride is a protoberberine with strong anticancer activity. It can be used to prepare Coralyne derivatives, a fluorescent DNA-based molecular rectifier built into DNA duplexes through site-specific insertion. It acts as a topoisomerase I toxic molecule, inducing topoisomerase I-mediated DNA cleavage.

STAT5-IN-2 is an inhibitor of STAT5 with antileukemic effects (EC50s: 9 μM and 5 μM in K562 and KU812 cells, respectively).

9-Hydroxyellipticine hydrochloride is an inhibitor of Topo II and RyR, exhibiting antitumor, antioxidant, and catecholamine-releasing activities. It inhibits Hela S-3 and 293T cells with IC50s of 1.6 μM and 1.2 μM, respectively.

Enocitabine is a nucleoside analog. Enocitabine inhibits the replication of human cytomegalovirus(HCMV) and it also has antileukemic and antiviral activities. Enocitabine is also a potent DNA replication inhibitor and a DNA chain terminator.

Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg mL in a panel of different tumors).

PD166326, a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, demonstrates antileukemic activity with IC50 values of 6 nM for Src and 8 nM for Abl. [1] [2].

KPT-251 is a selective nuclear export inhibitor.

Moflomycin is an anthracycline derivative. It exhibits a higher antileukemic activity compared to other anthracyclines.

5,10-Dideazaaminopterin is an antileukemic drug.

5,10-Dideazafolic acid is an antileukemic drug.

Botryodiplodin, an antibiotic, has antileukemic activity from Botryodiplodia theobromae. It has the property of turning the skin of the individual in various shades of pink 2-3 hrs after application. It is a toxic metabolite of Penicillium carneo-lutescen

Hisphen shows antileukemic activity.

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

Mezerein is a chemical compound with antileukemic properties and acts as a PKC activator. It effectively inhibits the growth of yeast expressing PKC alpha (IC 50 = 1190 nM), PKC beta1 (IC 50 = 908 nM), and PKC delta (IC 50 = 141 nM). However, it does not inhibit the growth of yeast expressing PKC.

Idarubicin, a potent anthracycline antileukemic agent, is orally active in its application. It functions by inhibiting topoisomerase II, thus interfering with DNA replication and RNA transcription. Furthermore, Idarubicin induces DNA damage, inhibits DNA synthesis, and suppresses c-myc expression. It also demonstrates inhibitory effects on the growth of bacteria and yeasts [1] [2] [3] [4] [5].

1. Triptonide (PG 492) is effective in the treatment of autoimmune diseases and has potent antileukemic and antitumor activities. 2. Triptonide possesses anti-inflammatory activity, upregulate the expression of IL-37, and this expression was suppressed by ERK1 2 and p38 MAPK inhibitors.

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys) is an anticarcinogenic agent that exhibits antileukemic activity by inhibiting DNA synthesis in HL60 cells [1] and acts as an inhibitor of P450 [2].

GCN2iB is a GCN2 inhibitor. GCN2iB may be useful for the treatment of cancer. The inhibition of GCN2 sensitizes cancer cells with low basal-level expression of asparagine synthetase (ASNS) to the antileukemic agent L-asparaginase (ASNase) in vitro and in vivo.

AZD-1897 is a highly efficient ATP-competitive pan-PIM inhibitor with anticancer and antileukemic activity, inhibiting PIM1, PIM2, and PIM3, which can be used to study multiple myeloma.

HDAC-IN-49 is a potent, non-selective inhibitor of HDAC (HDAC), demonstrating IC50 values of 13 nM for HDAC1, 14 nM for HDAC2, 21 nM for HDAC3, 1880 nM for HDAC4, and 10 nM for HDAC6. This compound exhibits significant antileukemic activity while maintaining low cytotoxicity towards healthy cells.

(+)SHIN2, an isomer of (-)SHIN2, is an inhibitor of serine hydroxymethyltransferase (SHMT) with antileukemic effects and shows synergistic activity with Methotrexate in in vivo xenotransplantation models [1].