A study of the effects imidazolium-based ionic liquids on 60 human cancer cell lines representing diverse histologies has identified four compounds which show potency at a nanomolar dose.

Piperidone-sulphonamide and curcumin based molecular hybrids were synthesised, which showed anti-cancer activity on 60 human tumor cell line panels their inhibitory effect due to apoptosis.

We describe a novel strategy to increase the selective toxicity of genotoxic compounds. The involves synthesis bifunctional molecules capable forming DNA adducts that have high affinity for specific proteins in target cells. It is proposed association such with damaged sites can compromise protein function and/or repair resulting increased toxicity. compound consisting an aniline mustard linked 7α position estradiol. This form covalent estrogen receptor. Breast cancer cells express levels...

We analyzed bladder DNA from 27 cancer patients for dG-C8-4-aminobiphenyl (dG-C8-ABP) adducts using the liquid chromatography tandem mass spectrometry method with a 700 attomol (1 adduct in 10(9) bases) detection limit. Hemoglobin (Hb) 4-aminobiphenyl (4-ABP) levels were measured by gas chromatography-mass spectrometry. After isolation of dG-C8-ABP immunoaffinity and further purification, deuterated (d9) (MW=443 Da) was added to each sample. Structural evidence quantification determined...

Novel hybrids exhibiting excellent anticancer activity against most of the NCI 60 cell lines through apoptotic pathways are reported herein.

In this study the potential for anticancer activity of 4-aminoquinoline-triazine based hybrids has been investigated on 60 human cancer cell lines (NCI 60). The representative compounds show a range and apoptosis as mode growth inhibition.

In this study, six curcuminoids containing a tert-butoxycarbonyl (Boc) piperidone core were successfully synthesized, five of them are novel compounds reported here for the first time. These prepared through an aldolic condensation by adding tetrahydropyranyl-protected benzaldehydes or substituted benzaldehyde to reaction mixture 4-Boc-piperidone and lithium hydroxide in alcoholic solvent. A 44–94% yield was obtained supporting developed methodology as good strategy synthesis chalcones....

A novel cyclolignanic quinone, 7-acetyl-3′,4′-didemethoxy-3′,4′-dioxopodophyllotoxin (CLQ), inhibits topoisomerase II (TOPO II) activity. The extent of this inhibition was greater than that produced by the etoposide quinone (EQ) or etoposide. Glutathione (GSH) reduces EQ and CLQ to their corresponding semiquinones under anaerobic conditions. latter were detected EPR spectroscopy in presence MgCl2 but not its absence. Semiquinone spectra change with quinone/GSH mol ratio, suggesting covalent...

Abstract The multifunctional molecule 11β-dichloro consists of a ligand for the androgen receptor linked to bifunctional alkylating group, permitting it create DNA adducts that bind receptor. We propose binding 11β-DNA acts both shield damaged sites from repair and disrupt expression genes essential growth survival. investigated formation in tumor xenograft nontumor tissues mice. Using [14C]-11β-dichloro, we show remains intact blood is widely distributed mouse after i.p. injection. Covalent...

Thyroid hormone resistance syndrome is characterized by a reduced target tissue response to the action of thyroid hormone, which leads high levels free thyroxine and triiodothyronine with non-suppressed thyrotropin (TSH). Recently, three cases papillary carcinoma associated were published. The main challenge in this situation difficulty maintaining suppression TSH without producing symptoms hyperthyroidism. We present another case an association carcinoma, we share our experience...

Human xylazine (XYL) abuse among addicts has received great interest due to its potential toxic effects upon and the need understand mechanism of action associated with health effects. XYL is an alpha-2 agonist restricted veterinarian applications, without human medical applications. Our previous work demonstrated that combination cocaine (COC) and/or 6-monoacetylmorphine (6-MAM) induce cell death through apoptotic mechanism. The aim this study was determine effect on generation reactive...

Phthalates have been used in a wide variety of consumer goods. Their versatility as plasticizers has translated into worldwide use vast array products. These compounds can leach matrices, such food and liquids that be routed for human exposure. One the most phthalates is Diethylhexyl phthalate (DEHP). its metabolite 2-ethyl-1-hexanol (2-EH) demonstrated biological effects which merit further evaluation. In this work, we expand on our previous work with DEHP screen 2-EH different cell death...

Etoposide is a chemotherapy drug derived from the natural lignin podophyllotoxin. Our novel generated Aza-podophyllotoxin compounds (AZP 8a & AZP 9a) are analogues of podophyllotoxin and were previously screened for anti-cancer activity through NCI 60 cell line screening panel showing on various types including colon cancer. This study expands toxicological by studying apoptosis hallmark events as part mechanism action these cancer cells. The COLO 205 was selected exposed to determine IC50...

Interest in DNA binding drugs has increased recent years due to their importance the treatment of genome-related diseases, like cancer. A new family water-soluble compounds, benzothiazolo[3,2-a]quinolinium chlorides (BQCls), is studied here as potential candidates for chemical solid tumor cells that may encounter low-oxygen environments, a condition known hypoxia. These compounds are good intercalators; however, no studies have been made these under hypoxic conditions. This work demonstrates...

Benzazolo[3,2-a]quinolium salts (BQS) are cationic quaternary alkaloids with similar structure to the anticancer agent ellipticine. This study describes synthesis and screen, at experimental concentration of 10 mM, utilizing 60 cell line anti-cancer screening two BQS, namely, 7-benzyl-3- aminobenzimidazo[3,2-a]quinolinium chloride (ABQ-48: NSC D-763307) corresponding nitrobenzimidazo[3,2-a]quinolinium (NBQ 48: D-763303). Compound ABQ-48: D-763307 was also screened in 5-dose NCI panel. These...

This study reports the capacity of three nitro substituted benzazolo[3,2-a]quinolinium salts NBQs: NBQ 95 (NSC-763304), 38 (NSC 763305), and 97 (NSC-763306) as potential antitumor agents. NBQ’s are unnatural alkaloids possessing a positive charge that could facilitate interaction with cell organelles. The anticancer activities these compounds were evaluated through National Cancer Institute (NCI) 60 line screening which represents diverse histologies. was performed at 10 μM on all lines....

Objectives: The present study evaluates novel cationic quinoline derivatives known as benzimidazo[3,2- a ]quinolinium salts (BQS) named NBQ-48 and ABQ-48 that have structural similarities to anti-cancer substances such ellipticine berberine. Methods: Toledo human lymphoma (ATCC CRL2631) cells were treated for 24 48 hours. Apoptosis related endpoints cell cycle arrest, mitochondrial damage, RNS ROS generation the activity of several apoptosis proteins caspases inducing factor (AIF) studied...

Abstract There is a continues need to develop technologies detect and characterize circulating tumor cells that can become aggressive, metastatic, hard treat. Among these aggressive CTC are known as Hypoxic cell populations learn adapt survive low oxygen levels. Our project aims test the applicability of novel technique Circulating Tumor Cells (H-CTC) move from tumors blood invading other tissues becoming resistant chemotherapy radiation. The proposed assay incorporates set patented organic...

This study presents the applicability of a novel nitro-substituted heterocyclic compound NBQ48, member family compounds identified as 3 nitrobenzazolo[3,2-a] quinolinium chloride salts (NBQS) screening tool to identify hypoxic tumor cells.The was tested on COLO 205 colon cancer cells 2D and 3D cultures treated with NBQ48 assess formation bio-reduction fluorescent metabolite under conditions in contrast, those aerobic environment.Hypoxic environment created applying controlled gas...