mitoxantrone

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

Mitoxantrone diacetate is a potent inhibitor of topoisomerase II. Mitoxantrone diacetate also inhibits protein kinase C (PKC) (IC50: 8.5 μM). Mitoxantrone diacetate exhibits antitumour effects and also has an antiorthopoxvirus effect, acting against bovine pox (EC50: 0.25 μM) and monkey pox (EC50: 0.8 μM).

BCRP-IN-2 is a compound with BCRP inhibitory activity, exhibiting enhanced inhibition of BCRP upon UV activation. It serves as a valuable probe for studying interactions between quinazoline amine derivatives and BCRP, and it stimulates ATP hydrolysis of the BCRP transporter, leading to increased mitoxantrone accumulation in BCRP-overexpressing H460 MX20 cells.

Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, functions as a topoisomerase II inhibitor and DNA intercalator, demonstrating anti-tumor activity [1] [2].

WEHI-150 is an analog of mitoxantrone, a DNA interstrand cross-linker (t1 2=12.5 h). WEHI-150 is capable of forming covalent adducts on CpG sequences, with a particular preference for methylated CpG sites. Formaldehyde-activated WEHI-150 induces DNA interstrand cross-linking and blocks transcription in a concentration-dependent manner. WEHI-150 mediates the formation of covalent adducts that do not interact with guanine N-2 and forms adducts on new DNA sequences.

Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerated and more effective at inhibiting tumor growth compared with mitoxantrone in a human xenograft tumor regression mouse model. Mechanistically, we found that ethonafide inhibited topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIalpha and -beta. In addition, ethonafide induced a potent G(2) cell cycle arrest in the DU 145 human prostate cancer cell line. By creating stable cell lines with decreased expression of topoisomerase IIalpha or -be......

Mono-Pal-MTO, a palm oil-derived lipid formed by integrating the anticancer agent mitoxantrone (MTO) with palmitoleic acid, exhibits enhanced anticancer activity and efficient siRNA cell delivery when its nanoparticles are mixed with those of di-Pal-MTO at a molar ratio of 1:1 [1].

Di-Pal-MTO, a lipid derivative synthesized from palm oil by integrating the anticancer agent mitoxantrone (MTO) with palmitoleic acid, exhibits enhanced anticancer activity and efficient siRNA cell delivery when nanoparticles of mono-Pal-MTO and di-Pal-MTO are combined at a molar ratio of 1:1 [1].

33-BCRP inhibitor is a compound that blocks the action of breast cancer resistance protein (BCRP), enhancing the susceptibility of mitoxantrone-resistant H460/MX20 lung cancer cells to the cytotoxic effects of mitoxantrone, both individually and when combined with UV radiation. Additionally, it enhances the sensitivity of KB-C2 epidermal carcinoma cells, which overexpress P-glycoprotein (P-gp) or multidrug resistance protein (MDR), to colchicine-induced apoptosis. Furthermore, at a concentration of 5 µM, it boosts the intracellular accumulation of mitoxantrone in H460/MX20 cells.

6,8-Diprenylnaringenin (Senegalensin) is a natural product from hop Humulus lupulus. 6,8-Diprenylnaringenin is a breast cancer resistance protein(BCRP) inhibitor with some estrogenicity.