Search results for: Ketan C. Ruparelia

Items from 1 to 10 out of 10 results

article

Analysis of plant secondary metabolism using stable isotope‐labelled precursors

Randolph R.J. Arroo, Avninder S. Bhambra, Christophe Hano, Gülin Renda, more

Phytochemical Analysis > 32 > 1 > 62 - 68

Introduction Analysis of biochemical pathways typically involves feeding a labelled precursor to an organism, and then monitoring the metabolic fate of the label. Initial studies used radioisotopes as a label and then monitored radioactivity in the metabolic products. As analytical equipment improved and became more widely available, preference shifted the use stable ‘heavy’ isotopes like deuterium...

article

Flavones as tyrosinase inhibitors: kinetic studies in vitro and in silico

Randolph R.J. Arroo, Suat Sari, Burak Barut, Arzu Özel, more

Phytochemical Analysis > 31 > 3 > 314 - 321

Introduction Tyrosinase is a multifunctional copper‐containing oxidase enzyme that catalyses the first steps in the formation of melanin pigments. Identification of tyrosinase inhibitors is of value for applications in cosmetics, medicine and agriculture. Objective To develop an analytical method that allows identification of drug‐like natural products that can be further developed as tyrosinase...

article

(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent

Neill J. Horley, Kenneth J.M. Beresford, Supriya Kaduskar, Prashant Joshi, more

Bioorganic & Medicinal Chemistry Letters > 2017 > 27 > 24 > 5409-5414

The overexpression of CYP1 family of enzymes is reported to be associated with development of human carcinomas. It has been well reported that CYP1A1 specific inhibitors prevents carcinogenesis. Herein, thirteen pyridine-4-yl series of chalcones were synthesized and screened for inhibition of CYP1 isoforms 1A1, 1B1 and 1A2 in Sacchrosomes™ and live human HEK293 cells. The structure-activity relationship...

article

Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines

Neill J. Horley, Kenneth J.M. Beresford, Tarun Chawla, Glen J.P. McCann, more

European Journal of Medicinal Chemistry > 2017 > 129 > C > 159-174

The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of synthetic pyridylchalcones. They inhibit human CYP1B1 enzyme bound to yeast-derived microsomes (Sacchrosomes™) with IC₅₀ values of 10 and 9 nM, respectively, and show a very high level...

article

Synthesis and antitrypanosomal activities of novel pyridylchalcones

Avninder S. Bhambra, Ketan C. Ruparelia, Hoon L. Tan, Deniz Tasdemir, more

European Journal of Medicinal Chemistry > 2017 > 128 > C > 213-218

A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC₅₀ value of 0.29 μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani...

article

Petals of Crocus sativus L. as a potential source of the antioxidants crocin and kaempferol

Keti Zeka, Ketan C. Ruparelia, Maria A. Continenza, Dimitrios Stagos, more

Fitoterapia > 2015 > 107 > C > 128-134

Saffron from the province of L'Aquila, in the Abruzzo region of Italy, is highly prized and has been awarded a formal recognition by the European Union with EU Protected Designation of Origin (PDO) status. Despite this, the saffron regions are abandoned by the younger generations because the traditional cultivation of saffron (Crocus sativus L.) is labour intensive and yields only one crop of valuable...

article

Phytoestrogens as natural prodrugs in cancer prevention: towards a mechanistic model

Randolph R. J. Arroo, Kenneth Beresford, Avninder S. Bhambra, Mike Boarder, more

Phytochemistry Reviews > 2014 > 13 > 4 > 853-866

It has been widely acknowledged that regular consumption of fresh fruits and vegetables is linked with a relatively low incidence of cancers (e.g. breast, cervix, and colon). Notably, dietary polyphenolic compounds that show some structural similarity to human estrogen, e.g. isoflavones, coumestans, lignans, flavones, have been proposed to play a role in cancer prevention. However, at present there...

article

Anticancer effects of the metabolic products of the resveratrol analogue, DMU-212: Structural requirements for potency

Vasilis P. Androutsopoulos, Ketan C. Ruparelia, Athanasios Papakyriakou, Harilaos Filippakis, more

European Journal of Medicinal Chemistry > 2011 > 46 > 6 > 2586-2595

The methoxylated trans-stilbene resveratrol analogue, (E)-3,4,5,4′-tetramethoxystilbene (1), has shown promising antiproliferative activity in in vitro cell line and in vivo models. In vivo 1 gives rise to several metabolic products through demethylation or hydroxylation reactions at the stilbene moiety. In the present study we examined the anticancer activity of 1 and the metabolites (E)-3′-hydroxy-3,4,5,4′-tetramethoxystilbene...

article

Synthesis and Biological Evaluation of Novel Chloroethylaminoanthraquinones with Potent Cytotoxic Activity against Cisplatin-Resistant Tumor Cells

Klaus Pors, Zennia Paniwnyk, Ketan C. Ruparelia, Paul H. Teesdale-Spittle, more

Journal of Medicinal Chemistry > 2004 > 47 > 7 > 1856 - 1859

article

Anthraquinone-peptides as inhibitors of AP-1 transcription factor

Taeeba Ijaz, Phoung Tran, Ketan C. Ruparelia, Paul H. Teesdale-Spittle, more

Bioorganic & Medicinal Chemistry Letters > 2001 > 11 > 3 > 351-353

Peptide-1-[N-{2-succinamidylethyl}amino]anthraquinones containing five–seven amino acid residues including the KCR motif important in AP-1 protein binding to DNA have been synthesised as potential transcription factor inhibitors. These anthraquinone-peptides showed DNA intercalative binding and inhibition of AP-1 protein binding to its DNA consensus sequence.

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Search results for: Ketan C. Ruparelia

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