ORCID Profile
0000-0002-6932-3188
Current Organisations
The University of Auckland
,
Harran University Faculty of Agriculture
,
University of Hertfordshire
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Publisher: CSIRO Publishing
Date: 2002
DOI: 10.1071/AR01133
Abstract: The salt tolerance of 25 cowpea genotypes (Vigna unguiculata L. Walp.) was studied during early vegetative growth. Salinity treatments were applied by irrigating with a nutrient solution containing 0, 85, and 170 mmol NaCl/L. Seedling survival decreased linearly as salinity increased, but this enabled cowpea genotypes to be ranked for salinity tolerance according to the magnitudes of slopes of regression of survival percentage on salinity. Sodium concentration was higher in roots than in shoots in all genotypes, and increased significantly in both roots and shoots as salinity increased. Chloride concentration in both roots and shoots increased with increasing salinity in all genotypes, and was higher in shoots than in roots at 85 and 170 mmol NaCl/L. In some cases, Ca, Mg, K, and P concentrations were reduced by an increase in salinity, but none of the genotypes appeared to suffer any nutrient deficiency. We observed wide differences in responses to salinity, and our results suggest that during the growth stage studied, 7 of the 25 genotppes tested could be classified as tolerant or relatively tolerant to salinity (Sonorense, CB3, CB27, Cuarenteño, CB46, Paceño, and IT82D-889).
Publisher: Informa UK Limited
Date: 14-05-2021
Publisher: Royal Society of Chemistry (RSC)
Date: 2014
DOI: 10.1039/C3MD00320E
Publisher: Royal Society of Chemistry (RSC)
Date: 2019
DOI: 10.1039/C9MD00305C
Abstract: Close-shelled carbocations DNA intercalators Pr-ADOTA and Pr-DAOTA are very cytotoxic against the cancer cell lines MDA-MB-231 (breast) and HCT116 (colon).
Publisher: Elsevier BV
Date: 12-2006
Publisher: MDPI AG
Date: 06-01-2023
DOI: 10.3390/IJMS24021167
Abstract: Dibenzylbutyrolactone lignans (DBLs) are a class of natural products with a wide variety of biological activities. Due to their potential for the development of human therapeutic agents, DBLs have been subjected to various SAR studies in order to optimise activity. Previous reports have mainly considered changes on the aromatic rings and at the benzylic carbons of the compounds, whilst the effects of substituents in the lactone, at the C-9′ position, have been relatively unexplored. This position has an unexploited potential for the development of novel dibenzyl butyrolactone derivatives, with previous preliminary findings revealing C-9′-hydroxymethyl analogues inducing programmed cell cycle death. Using the core structure of the bioactive natural product arctigenin, C-9′ derivatives were synthesised using various synthetic pathways and with prepared derivatives providing more potent anti-proliferative activity than the C-9′-hydroxymethyl lead compound.
Publisher: Informa UK Limited
Date: 23-03-2023
Publisher: Future Science Ltd
Date: 02-2023
Abstract: Background: It has been demonstrated that the lead compound 2-phenylimidazo[1,2- a]quinoline 1a selectively inhibits CYP1 enzymes. Additionally, CYP1 inhibition has been linked to inducing antiproliferative effects in various breast cancer cell lines as well as relieving drug resistance caused by CYP1 upregulation. Materials & methods: Herein, 54 novel analogs of 2-phenylimidazo[1,2- a]quinoline 1a have been synthesized with varied substitution on the phenyl and imidazole rings. Antiproliferative testing was conducted using 3 H thymidine uptake assays. Results: 2-Phenylimidazo[1,2- a]quinoline 1a and phenyl-substituted analogs 1c (3-OMe), 1n (2,3-napthalene) displayed excellent anti-proliferative activities, demonstrating their potency against cancer cell lines for the first time. Molecular modeling suggested that 1c and 1n bind similarly to 1a in the CYP1 binding site.
Publisher: Elsevier BV
Date: 05-2023
Publisher: Elsevier BV
Date: 2017
DOI: 10.1016/J.BMCL.2016.12.009
Abstract: 3-Amino-2-arylcarboxamide-thieno[2,3-b]pyridines are a known class of antiproliferative compounds with activity against the phospholipase C enzyme. To further investigate the structure activity relationships of these derivatives a series of analogues were prepared modifying key functional groups. It was determined that modification of the 3-amino and 2-aryl carboxamide functionalities resulted in complete elimination of activity, whilst modification at C-5 allowed compounds of greater activity to be prepared.
Publisher: MDPI AG
Date: 26-10-2021
Abstract: Inhibition of phosphatidylcholine-specific phospholipase C (PC-PLC) has previously been shown to be a potential target for novel cancer therapeutics. One downstream consequence of PC-PLC activity is the activation of NF-κB, a nuclear transcription factor responsible for transcribing genes related to oncogenic traits, such as proliferation, angiogenesis, metastasis, and cancer cell survival. Another biological pathway linked to NF-κB is the exogenous delivery of nitric oxide (NO), which decreases NF-κB activity through an apparent negative-feedback loop. In this study, we designed and synthesised 13 novel NO-releasing derivatives of our previously reported class of PC-PLC inhibitors, 2-morpholinobenzoic acids. These molecules contained a secondary benzylamine group, which was readily nitrosylated and subsequently confirmed to release NO in vitro using a DAF-FM fluorescence-based assay. It was then discovered that these NO-releasing derivatives possessed significantly improved anti-proliferative activity in both MDA-MB-231 and HCT116 cancer cell lines compared to their non-nitrosylated parent compounds. These results confirmed that the inclusion of an exogenous NO-releasing functional group onto a known PC-PLC inhibitor enhances anti-proliferative activity and that this relationship can be exploited in order to further improve the anti-proliferative activity of current/future PC-PLC inhibitors.
Publisher: CSIRO Publishing
Date: 2023
DOI: 10.1071/FP23060
Publisher: Royal Society of Chemistry (RSC)
Date: 2014
DOI: 10.1039/C3MD00290J
Publisher: Springer Science and Business Media LLC
Date: 23-06-2021
Publisher: Royal Society of Chemistry (RSC)
Date: 2021
DOI: 10.1039/D0AY02208J
Abstract: In this manuscript, we report our work in the development and optimisation of a MALDI-TOF mass spectrometry assay to monitor the kinetics and inhibition of PC-PLC, a phospholipase that catalyses the hydrolysis of phosphatidylcholines.
Publisher: Wiley
Date: 28-07-2004
Publisher: MDPI AG
Date: 26-11-2021
DOI: 10.3390/PHARMACEUTICS13122020
Abstract: The compounds 2-amino-3-carboxamido-thieno[2,3-
Publisher: MDPI AG
Date: 27-01-2022
DOI: 10.3390/MOLECULES27030836
Abstract: 3-Amino-2-arylcarboxamido-thieno[2,3-b]pyridines have been shown to have anti-proliferative activity, but are also known to have poor solubility. This has been previously proposed to be due to their extensive planarity, which allows for intermolecular stacking and crystal packing. We herein report the synthesis of fifteen novel thieno[2,3-b]pyridines that have incorporated bulky, but easily cleavable, ester and carbonate functional groups in an effort to decrease crystal packing. The addition of these ‘prodrug-like’ moieties into the thieno[2,3-b]pyridine resulted in compounds with increased activity against HCT-116 colon cancer cells and the triple-negative breast cancer cell line MDA-MB-231.
Publisher: Elsevier BV
Date: 07-2016
DOI: 10.1016/J.BMCL.2016.05.026
Abstract: A series of pyrrole analogues of combretastatin (CA-4) were synthesized and tested for their anti-proliferative activity. The highly diastereoselective acyl-Claisen rearrangement was used to provide 2,3-syn disubstituted morpholine amides which were used as precursors for the various analogues. This synthesis allows for the preparation of 1,2- and 2,3-diaryl-1H-pyrroles which are both geometrically similar to CA-4. These pyrrolic analogues were tested for their anti-proliferative activity against two human cell lines, K562 and MDA-MB-231 with 2,3-diaryl-1H-pyrrole 35 exhibiting the most potent activity with IC50 value of 0.07μM against MDA-MB-231 cell line.
Publisher: MDPI AG
Date: 13-07-2023
Abstract: 3-Amino-2-arylcarboxamido-thieno[2-3-b]pyridines have been previously described as having potent anti-proliferative activity against MDA-MB-231 and HCT116 cancer cell lines. The mechanism by which these molecules prevent cancer cell growth is proposed to be through interfering with phospholipid metabolism via inhibition of PI-PLC, along with other cellular processes. Previously, 5-cinnamyl derivatives of these thieno[2-3-b]pyridines have been shown to have enhanced anti-proliferative activity compared to compounds lacking this moiety, indicating a tethered aromatic ring is important for this western region of the pharmacophore. Herein, we report the synthesis and biological evaluation of a library of 40 novel thieno[2-3-b]pyridine analogues containing shorter benzoyl or secondary benzyl alcohol tethers at the 5-position, in addition to various substituents on the two phenyl rings present on the molecule. Compounds bearing alcohol functionality had improved efficacy compared to their benzoyl counterparts, in addition to a 2-methyl-3-halogen substitution on the 2-arylcarboxamide ring being important for maximising anti-proliferative activity. The most potent molecules 7h and 7i demonstrated IC50 concentrations of 25–50 nM against HCT116 and MDA-MB-231 cells, a similar level of activity as previous thienopyridine compounds bearing cinnamyl moieties, suggesting that these novel derivatives with shorter tethers were able to maintain potent anti-proliferative activity, while allowing for a more concise synthesis.
Publisher: Royal Society of Chemistry (RSC)
Date: 2022
DOI: 10.1039/D2OB00336H
Abstract: A flexible approach to C7 keto dibenzyl butyrolactone lignans was developed and the synthesis of several natural products and their related derivatives is described herein. The developed pathway proceeds through enantioenriched β-substituted butyrolactones, from which facile aldol addition and subsequent oxidation affords the desired benzylic ketone moiety. This methodology was used to complete the first enantioselective total syntheses of three natural products, (+)-7-oxohinokinin, (+)-7-oxoarcitin and (+)-conicaol B, and a further five analogues. The utility of this method was further demonstrated through a 1-2 step modification to access another class of natural product, aryltetralin lignans, allowing the asymmetric total synthesis of (-)-isopolygamain and a polygamain derivative. Anti-proliferative testing determined (-)-isopolygamain was the most active of the compounds prepared, with IC
Publisher: Springer Science and Business Media LLC
Date: 10-03-2016
Publisher: Springer Science and Business Media LLC
Date: 04-04-2012
Publisher: MDPI AG
Date: 14-03-2021
DOI: 10.3390/MOLECULES26061608
Abstract: Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.
Location: United Kingdom of Great Britain and Northern Ireland
No related grants have been discovered for Euphemia Leung.