3-methoxy aroylhydrazones – free radicals scavenging, anticancer and cytoprotective potency

Hristova-Avakumova, Nadya; Yoncheva, Krassimira; Nikolova-Mladenova, Boryana; Traykov, T.; Momekov, Georgi; Hadjimitova, Vera

doi:10.1080/13510002.2016.1276256

Cited by 14 publications

(9 citation statements)

References 32 publications

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“…In this case, the IC 50 value of 11 was 14.46 mmol/L and the IC 50 value of C was 19.11 mmol/L (whereas the respective value of Ox was 2.39 mmol/L). These results are comparable with previously reported activities of aroylhydrazones [32]. Hristova-Avakumova et al [32] investigated the cytotoxic activity of 3-methoxy aroylhydrazone on HepG2 (hepatocellular carcinoma cell line), HEK-293 (human Table 1.…”

Section: Resultssupporting

confidence: 89%

“…These results are comparable with previously reported activities of aroylhydrazones [32]. Hristova-Avakumova et al [32] investigated the cytotoxic activity of 3-methoxy aroylhydrazone on HepG2 (hepatocellular carcinoma cell line), HEK-293 (human Table 1. Antiproliferative activity of the hydrazones on MCF-7, MDA-MB-231 and MCF-10A cells after 72 h of treatment (MTT-dye reduction assay).…”

Section: Resultssupporting

confidence: 89%

“…All obtained hydrazones were characterized by standard analytical procedures (UV/VIS, NMR, MS, HPLC, X-ray) [34,[37][38][39][40][41][42]. The physico-chemical properties of the compounds 1-12 were investigated and reported [32,36,38,39,41].…”

Section: Chemistrymentioning

confidence: 99%

“…For example, one of the compounds, salicylaldehyde benzoylhydrazone (SBH), has been shown to inhibit DNA synthesis and cell growth in a variety of cultured human and rodent cells [25]. Various derivatives of SBH with a number of functional groups have been created in recent years, in order to discover new bioactive compounds with high antitumour activity and minimal toxicity [26][27][28][29][30][31][32][33].…”

Section: Introductionmentioning

confidence: 99%

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Cancer cell growth inhibition by aroylhydrazone derivatives

Илиев

Kontrec

Detcheva

et al. 2019

Biotechnology & Biotechnological Equipment

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Hydrazones have versatile properties that make them promising for a range of possible applications. In this study, we examined a library of 17 aroylhydrazones derived from nicotinic acid hydrazide (1-12) and isonicotinic acid hydrazide (A-E) created by us for their biological activity. The antiproliferative activity of the compounds was investigated on non-tumour MCF-10A cells and cancer cell lines, MCF-7 and MDA-MB-231. Four compounds were selected as most active in cell growth inhibition of the tumour cell lines. These compounds, 5, 11, C and E, were tested on four additional cell lines: non-tumour BJ and cancer cell lines, HeLa, HepG2 and HT-29. Compounds 5 and E exhibited the highest selectivity index on cancer cell lines MDA-MB-231, HeLa and HepG2. High selectivity to MCF-7 cells was demonstrated with compound 5. Compound C was very selective to HepG2 cells as well as to MDA-MB-231 but to a lesser degree. Compound 11 showed selectivity against MDA-MB-231. The obtained results allow assessing the structure-activity relationship of the compounds and provide insight into the further development of this group of aroylhydrazones as more potent and selective anti-neoplastic agents.

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Section: Resultssupporting

confidence: 89%

Section: Resultssupporting

confidence: 89%

Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Cancer cell growth inhibition by aroylhydrazone derivatives

Илиев

Kontrec

Detcheva

et al. 2019

Biotechnology & Biotechnological Equipment

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“…Azomethine group (-NH-N=CH-) contained in their structure is connected with carbonyl group and is responsible for the different pharmacological applications of cited compounds. Hydrazid-hydrazones have, therefore, attracted considerable attention to their wide range of biological activities (Sarıgöl et al 2015), including antioxidant, anticancer and cytoprotective potency (Hristova-Avakumova et al 2017;Nikolaevskii et al 2012).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and preliminary hepatotoxicity evaluation of new caffeine-8-(2-thio)-propanoic hydrazid-hydrazone derivatives

Mitkov¹,

Kondeva-Burdina²,

Zlatkov³

2019

PHAR

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New series of caffeine-8-(2-thio)-propanoic hydrazid-hydrazone derivatives were designed and synthesized. The targed compounds were obtained in yields of 51 to 96% and their structures were elucidated by FTIR, 1H NMR, 13C NMR, MS and microanalyses. All of the compounds were found to be “drug-like” as they fulfill the criteria of drug-likeness, which includes the MDDR-like rule. The tested compounds were subjected to in silico prediction of substrate/metabolite specificity and Drug Induced Liver Injury (DILI). The prediction for indicated that the evaluated compounds would most probably act as CYP1A2 substrates. The performed in vitro studies didn’t reveal statistically significant hepatotoxicity of the tested compounds, probably due to the pro-oxidant effects expressed on sub-cellular (isolated rat liver microsomes) level. The obtained experimental results confirmed the predicted low hepatotoxicity for the tested structures. Based on these results the compounds may be considered as promising structures for design of future molecules with low hepatotoxicity.

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