scholarly journals Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products

Molbank ◽  
10.3390/m1307 ◽  
2021 ◽  
Vol 2022 (1) ◽  
pp. M1307
Author(s):  
Dmitrii A. Aksenov ◽  
Alexander V. Aksenov ◽  
Lidiya A. Prityko ◽  
Nicolai A. Aksenov ◽  
Liliya V. Frolova ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Hydroxamic Acid ◽  
Methyl Esters ◽  
Hydroxamic Acids ◽  
Hela Cell Line ◽  
Lead Compounds

2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-methylation of hydroxamic acids. The cytotoxicity of these derivatives against the HeLa cell line was evaluated and found to be inferior compared to the parent lead compounds.

scholarly journals Synthesis, structural analysis, solution equilibria and biological activity of rhodium(iii) complexes with a quinquedentate polyaminopolycarboxylate

RSC Advances ◽  
2017 ◽  
Vol 7 (9) ◽  
pp. 5282-5296 ◽  
Author(s):  
Marija S. Jeremić ◽  
Hubert Wadepohl ◽  
Vesna V. Kojić ◽  
Dimitar S. Jakimov ◽  
Ratomir Jelić ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structural Analysis ◽  
Antitumor Activity ◽  
Hela Cell ◽  
Cell Line ◽  
Hela Cell Line ◽  
Solution Equilibria ◽  
Line P

Two new Rh(iii)–ed3a complexes [Rh(ed3a)(OH2)]·H2O and Na[Rh(ed3a)Cl]·H2O have shown good antitumor activity, especially against HeLa cell line.

Exploring the potential of imines as antiprotozoan agents with focus on t. Brucei and p. Falciparum

2018 ◽  
Author(s):  
◽  
Kola Augustus Oluwafemi
Keyword(s):  
Hela Cell ◽  
Cell Line ◽  
Special Focus ◽  
Hela Cell Line ◽  
Free Energies ◽  
Imino Group ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Pyridine Moiety ◽  
Nmr Study

This work focuses on the design, synthesis and evaluation of imine-containing heterocyclic and acyclic compounds with special focus on their bioactivity against parasitic protozoans (P. falciparum and T. brucei) - given the context of drug resistance in the treatment of malaria and Human African sleeping sickness and the fact that several bioactive organic compounds have been reported to possess the imino group. Starting from 2-aminopyridine, novel #-alkylated-5-bromo-7-azabenzimidazoles and substituted 5-bromo-1-(carbamoylmethy)-7-azabenzimidazole derivatives were prepared, and their bioactivity against parasitic protozoans was assessed. NMR spectra of the substituted 5- bromo-1-(carbamoylmethy)-7-azabenzimidazole derivatives exhibited rotational isomerism, and a dynamic NMR study was used in the estimation of the rate constants and the free- energies of activation for rotation. The free-energy differences between the two rotamers were determined and the more stable conformations were predicted. Novel 2-phenyl-7-azabenzimidazoles were also synthesised from 2-aminopyridine. A convenient method for the regioselective formylation of 2,3-diaminopyridines into 2-amino- 7-(benzylimino)pyridine analogues of 2-phenyl-7-azabenzimidazole was developed, and some of the resulting imino derivatives were hydrogenated to verify the importance of the imino moiety for bioactivity. The 2-phenyl-7-azabenzimidazoles and the 2-amino-7- (benzylimino)pyridine analogues were screened for their anti-protozoal activity and their cytotoxicity level was determined against the HeLa cell line. In order to validate the importance of the pyridine moiety, novel #-(phenyl)-2- hydroxybenzylimines, #-(benzyl)-2-hydroxybenzylimines and (±)-trans-1,2-bis[2- hydroxybenzylimino]cyclohexanes were also synthesized and screened for activity against the parasitic protozoans and for cytotoxicity against the HeLa cell line. The biological assay results indicated that these compounds are not significantly cytotoxic and a good number of them show potential as lead compounds for the development of new malaria and trypanosomiasis drugs.

scholarly journals Novel C-ring Analogs of Ursolic acid: Synthesis and Cytotoxic Evaluation

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Uppuluri V. Mallavadhani ◽  
Banita Pattnaik ◽  
Nitasha Suri ◽  
Ajit K. Saxena
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Ursolic Acid ◽  
Parent Compound ◽  
Acid Synthesis ◽  
Hela Cell Line ◽  
Hela Cell Lines ◽  
Protective Groups

Ursolic acid (1), a natural pentacyclic triterpenic acid, afforded a variety of ring-C transformed products (5–11) when treated with N-bromosuccinimide under the influence of a range of protective groups and solvents. The synthesized compounds have been evaluated for cytotoxic activity against prostate PC 3, leukemia THP 1, cervical Hela and lung A-549 cancer cell lines. Among the tested analogs, compounds 5, 8, 9 and 10 showed potent activity against PC 3, THP 1 and Hela cell lines. Especially, compound 10 showed enhanced activity against the Hela cell line than the parent compound. Compounds 5, 8 and 9 showed comparable activities against PC 3 and THP 1 cell lines.

scholarly journals New Secodaphnane-Type Alkaloids with Cytotoxic Activities from Daphniphyllum angustifolium Hutch

2021 ◽  
Author(s):  
Qing-Yun Lu ◽  
Jia-Hui Zhang ◽  
Ying-Yao Li ◽  
Xue-Xue Pu ◽  
Cui-Shan Zhang ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Natural Product ◽  
Cell Line ◽  
Cytotoxic Activities ◽  
Spectroscopic Methods ◽  
Hela Cell Line

AbstractOne new Daphniphyllum alkaloid, daphnioldhanol A (1), together with three known ones, were isolated from the stem part of Daphniphyllum angustifolium Hutch. Their structures were elucidated by spectroscopic methods and comparing with the literature data. Compound 2 is a new natural product, but known by synthesis as a racemate. Compound 1 exhibited week cytotoxic activity against Hela cell line with IC50 of 31.9 μM. Graphic Abstract

scholarly journals Cytotoxicity of ((E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one)) on HeLa cell line

2020 ◽  
Vol 1 (2) ◽  
Author(s):  
Adisty Ridha Damasuri ◽  
Eti Nurwening Sholikhah ◽  
Mustofa
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Colorimetric Assay ◽  
Cancer Cell Line ◽  
Positive Control ◽  
Probit Analysis ◽  
Hela Cell Line ◽  
Chalcone Derivatives ◽  
Cell Line Hela

In our previous study, some amino chalcone derivatives have been synthesized and evaluated their cytotoxicity against breast cancer cell line T47D. Among 11 amino chalcone derivatives, ((E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one)) exhibited the most active compound.This study aimed to investigate cytotoxic activity of the ((E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one)) against cervical cell line (HeLa). The cytotoxic activitywas determined using the MTT colorimetric assay. Cisplatin was used as positive control. From this MTT method, inhibitory concentration 50% (IC50) values were determined by probit analysis based on the relationship between log concentrations versus the percentage of cells growth inhibition.The results showed that the IC50 of ((E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one)) and cisplatinwere 22.75 ± 19.13 μg/mL and 14.96±1.08 μg/mL, respectively. In conclusion, the ((E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one)) has moderate cytotoxic activity against HeLa cell line based on National Cancer Institute (NCI) criteria.

scholarly journals ANTICANCER ACTIVITY OF CALANONE ON HeLa CELL LINE

2010 ◽  
Vol 10 (2) ◽  
pp. 240-244 ◽  
Author(s):  
Heny Ekowati ◽  
Indwiani Astuti ◽  
Mustofa Mustofa
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cervical Carcinoma ◽  
Carcinoma Cell ◽  
Suppressor Gene ◽  
Positive Control ◽  
Hela Cell Line ◽  
P53 Expression

Calanone (coumarin derivate compound), isolated from Calophyllum sp. had been shown to have cytotoxic activity on leukemia L1210 cell line with IC50 = 59.40 mg/mL. Calanone presumed have anticancer activity on HeLa cervical carcinoma cell. This study was conducted to investigate the cytotoxic and apoptotic activity of calanone and its effect to p53 and p21 expression on HeLa cervical carcinoma cell. Cytotoxic assay of calanone was performed on HeLa cell line, using MTT assay. Apoptotic assay was performed on HeLa cell line incubated with calanone for 24 h, by immunofluororescence method, using fluorochromes ethidium bromide and acridine orange. Expression of p53 was examined on HeLa cell line, by PCR with p53 wild-type primer. Expression of p21 was examined on HeLa cell line, by immunohistochemistry method. 5-fluorourasil was used as positive control in cytotoxic, apoptotic assay, and p53 expression. The result showed that calanone has cytotoxic activity on HeLa cell line, with IC50 = 22.887 mg/mL, caused cytotoxicity through apoptotic mechanism, increase p53 tumor suppressor gene expression, while the p21 expression test showed a negative result.   Keywords: Calanone, cytotoxic, HeLa cell line

Apoptosis induction of oroxylin A in human cervical cancer HeLa cell line in vitro and in vivo

Toxicology ◽  
2009 ◽  
Vol 257 (1-2) ◽  
pp. 80-85 ◽  
Author(s):  
Hua-Nan Li ◽  
Fei-Fei Nie ◽  
Wei Liu ◽  
Qin-Sheng Dai ◽  
Na Lu ◽  
...  
Keyword(s):  
Cervical Cancer ◽  
Hela Cell ◽  
Cell Line ◽  
Apoptosis Induction ◽  
Hela Cell Line ◽  
Oroxylin A ◽  
Human Cervical Cancer
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