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| 3. |
- Bravo, L, et al.
(författare)
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- 2021
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swepub:Mat__t
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| 4. |
- Tabiri, S, et al.
(författare)
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- 2021
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swepub:Mat__t
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| 5. |
- Glasbey, JC, et al.
(författare)
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- 2021
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swepub:Mat__t
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| 8. |
- Abdallah, Qasem M. A., et al.
(författare)
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Minor structural modifications to alchemix influence mechanism of action and pharmacological activity
- 2012
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Ingår i: Biochemical Pharmacology. - : Elsevier BV. - 0006-2952 .- 1356-1839 .- 1873-2968. ; 83:11, s. 1514-1522
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Tidskriftsartikel (refereegranskat)abstract
- Alchemix is an exemplar of a class of anthraquinone with efficacy against multidrug resistant tumours. We have explored further the mechanism of action of alchemix and investigated the effect of extending its side arm bearing the alkylating functionality with regard to DNA binding and activity against multidrug resistant cancer cells. Increasing the distance between the intercalating chromophore and the alkylating functionality of ICT2901 (propyl), ICT2902 (butyl) and ICT2903 (pentyl), led to a higher number of DNA alkylation sites, more potent topoisomerase II inhibition and generated more apoptotic and necrotic cells when analysed in p53-proficient HCT116 cells. Intriguingly, alchemix, the compound with the shortest distance between its intercalative chromophore and alkylating functionality (ethyl), did not conform to this SAR. A different toxicity pattern against DNA repair defective CHO cell lines as well as arrest of cells in Cl supports a somewhat distinct mode of action by alchemix compared with its analogues. Importantly, both alchemix and ICT2901 demonstrated greater cytotoxic activity against anthraquinone-resistant MCF-7/adr cells than wild-type MCF-7 cells. Subtle synthetic modification in this anthraquinone series has led to significant changes to the stability of DNA-compound complexes and cellular activity. Given that the failure of chemotherapy in the clinic is often associated with MDR, the results of both alchemix and ICT2901 represent important advances towards improved therapies.
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- Ahmad, Hafed Qasem, et al.
(författare)
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Assessment of Spatiotemporal Variability of Meteorological Droughts in Northern Iraq Using Satellite Rainfall Data
- 2021
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Ingår i: KSCE Journal of Civil Engineering. - : Korean Society Of Civil Engineers-KSCE. - 1226-7988 .- 1976-3808. ; 25:11, s. 4481-4493
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Tidskriftsartikel (refereegranskat)abstract
- The absence of a dense rainfall monitoring network and longer period data are the major hindrances of hydroclimatic study in arid and semi-arid regions. An attempt has been made for the evaluation of spatiotemporal changes in droughts at the northern semi-arid region of Iraq for the period 1981-2018 using high-resolution (0.05 degrees) precipitation data of Climate Hazards Group Infrared Precipitation with Stations (CHIRPS). The performance of CHIRPS in replicating rainfall and Standard Precipitation Index (SPI) for different timescales at eleven locations for the available period of observation data (2000-2014) was evaluated. The SPI was also used to estimate drought frequency and evaluate drought trends at all the CHIRPS grid points. A modified version of the non-parametric Mann-Kendall (MK) test was employed for a robust evaluation of the spatial distribution of temporal trends in droughts. The results showed a good ability of CHIRPS in reconstructing observed SPI with a correlation coefficient ranged from 0.64 to 0.87, BIAS between 1.05 and 1.81, Nash-Sutcliff efficiency from 0.39 to 0.55, and Willmott Index between 0.67 and 0.79. The CHIRPS also able to reconstruct the time series and probability distribution of observed SPI reasonably. Spatial distribution of droughts revealed a higher frequency of droughts of all categories and timescales in the east and north of Northern Iraq, mainly due to high rainfall variance. The MK test revealed a reduction in 6- and 12-month droughts in the northwest and an intensification at a few northeastern grids. It indicates droughts became more recurrent in the already drought-prone region and lessened in a less drought-prone region.
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