antileukemic

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.

ATH686 is an potent and selective Inhibitor of FLT3.

NL-1, a mitoNEET inhibitor, exhibits antileukemic effects.

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

ICCB280 was capable of inducing differentiation and apoptosis of ATRA-resistant patient blasts strongly signify that the activity of this compound can overcome resistance to other current therapies for AML with an unfavorable prognosis.

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.

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).

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

RUNX1/ETO-IN-1 is an inhibitor targeting the oncogenic fusion protein RUNX1-ETO, specifically affecting the NHR2 oligomerization domain. It binds directly to NHR2 (KD,app = 39 μM). By inducing apoptosis and promoting differentiation, RUNX1/ETO-IN-1 exhibits antileukemic activity in RUNX1/ETO translocation acute myeloid leukemia (AML) cells. Its near-neutral charge under physiological pH conditions grants it excellent cell membrane permeability.

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.