scholarly journals Sartoryglabrins, Analogs of Ardeemins, from Neosartorya Glabra

2011 ◽  
Vol 6 (6) ◽  
pp. 1934578X1100600
Author(s):  
Anake Kijjoa ◽  
Sonia Santos ◽  
Tida Dethoup ◽  
Leka Manoch ◽  
Ana Paula Almeida ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Human Tumor ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Growth Inhibitory ◽  
Nmr Spectrometry ◽  
Growth Inhibitory Activity ◽  
Mcf 7

Chemical investigation of a collection of the fungus Neosartorya glabra from Thailand furnished sartoryglabins A-C (1a, 1b and 2) which are analogs of the reverse prenylated indole alkaloids known as (-) ardeemins. Structures of these compounds were established by NMR spectrometry and an X-ray analysis. Sartoryglabins A-C were evaluated for their in vitro growth inhibitory activity on three human tumor cell lines: MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A375-C5 (melanoma). All the compounds exhibited strong to moderate activity against the MCF-7 cell line but weak or no activity against the NCI-H460 and A375-C5 cell lines. Sartoryglabin B was found to exhibit selectivity towards the MCF-7 cell line.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals Spiculisporic Acid E, a New Spiculisporic Acid Derivative and Ergosterol Derivatives from the Marine-Sponge Associated Fungus Talaromyces trachyspermus (KUFA 0021)

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Decha Kumla ◽  
Tida Dethoup ◽  
Suradet Buttachon ◽  
Narong Singburaudom ◽  
Artur M.S. Silva ◽  
...  
Keyword(s):  
Acid Derivative ◽  
Marine Sponge ◽  
Multidrug Resistant ◽  
Breast Adenocarcinoma ◽  
Gram Negative Bacteria ◽  
Small Cell Lung ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7

A new spiculisporic acid derivative, spiculisporic acid E (2), and a new natural product 3-acetyl ergosterol 5, 8-endoperoxide (1), were isolated, together with ergosta-4, 6, 8 (14), 22-tetraen-3-one, glaucanic acid and glauconic acid, from the culture of the marine-sponge associated fungus Talaromyces trachyspermus (KUFA 0021). All the compounds were inactive against Gram-positive and Gram-negative bacteria, and Candida albicans, as well as multidrug-resistant isolates from the environment. Spiculisporic acid E (2), glaucanic acid and glauconic acid did not show in vitro growth inhibitory activity against the MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A375-C5 (melanoma) cell lines by the protein binding dye SRB method.

scholarly journals Synthesis, characterization, molecular docking and in vitro anticancer activity of 3-(4-methoxyphenyl)-5-substituted phenyl-2-pyrazoline-1- carbothioamide

2021 ◽  
Vol 12 (2) ◽  
pp. 1648-1658
Author(s):  
Benupani Sahu ◽  
Rajapandi R ◽  
Avik Maji ◽  
Abhik Paul ◽  
Tanushree Singha ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Liver Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Hep G2 ◽  
Molegro Virtual Docker ◽  
Mcf 7

In the present study, eight numbers of new 3- (4-methoxy phenyl)-5-substituted phenyl-2-pyrazoline-1-carbothioamide (5a-h) have been synthesized from 1- (4-methoxy phenyl)-3- (substituted phenyl)-prop-2-en-1-one (3a-h) and structurally characterized by using FT-IR, 1H NMR, 13C NMR, Mass and Elemental analysis. The synthesized molecules were biologically evaluated for their in vitro anticancer activity against human breast adenocarcinoma (MCF-7), liver cancer (Hep-G2) and leukaemia cancer (K-562) cell line using Sulforhodamine B (SRB) bioassay technique. From the all synthesized compounds 5a, 5c, 5d, and 5e exhibited potent anticancer activity (GI50= <10µg/ml) as compared to the controlled drug 5-Fluorouracil (5-FU) (GI50=44.5µg/ml) and Adriamycin (ADR) (GI50= <10µg/ml) on MCF-7 cell lines. Besides this, all the synthesized compounds have exhibited moderate activity against human liver cancer (Hep-G2) and leukaemia cancer (K-562) cell lines. In addition, molecular docking studies were also explored in order to study the probable binding specificity into the active site of Epidermal Growth Factor Receptor tyrosine kinase (EGFR) (PDB ID: 1M17) using Molegro Virtual Docker Evaluation 2013 6.0.1 (MVD). Based on the molecular docking result, it was found that compound 5a exhibited the best interaction with the above target (i.e., EGFR) by interacting with specific amino acid residues such as: Thr 766, Gin 767, Thr 830, Cys 575, Ala 719 and Met 769.

scholarly journals Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF-7 and MDA-MB-231

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vincenza Barresi ◽  
Carmela Bonaccorso ◽  
Domenico A. Cristaldi ◽  
Maria N. Modica ◽  
Nicolò Musso ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Breast Cancer Cell Lines ◽  
Design And Synthesis ◽  
Human Breast Cell ◽  
Mcf 7

Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors. Based on the obtained results, we constructed a Volsurf+ (VS+) model using a dataset of 59 compounds able to predict the in vitro antitumor activity against MCF-7 cancer cell line for new derivatives. In the present paper, in order to further verify the robustness of this model, we report the results of the projection of more than 150 known molecules and 9 newly synthesized compounds. We predict their activity versus MCF-7 cell line and experimentally verify the in silico results for some promising chosen molecules in two human breast cell lines, MCF-7 and MDA-MB-231.

scholarly journals Synthesis and Biological Evaluation of Novel Triple-Modified Colchicine Derivatives as Potent Tubulin-Targeting Anticancer Agents

Cells ◽  
2018 ◽  
Vol 7 (11) ◽  
pp. 216 ◽  
Author(s):  
Urszula Majcher ◽  
Greta Klejborowska ◽  
Magdalena Kaik ◽  
Ewa Maj ◽  
Joanna Wietrzyk ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Binding Free Energy ◽  
3D Structure ◽  
Human Tumor ◽  
Biological Evaluation ◽  
Energy Estimates ◽  
Colchicine Derivatives ◽  
Mcf 7

Specific modifications of colchicine followed by synthesis of its analogues have been tested in vitro with the objective of lowering colchicine toxicity. Our previous studies have clearly shown the anticancer potential of double-modified colchicine derivatives in C-7 and C-10 positions. Here, a series of novel triple-modified colchicine derivatives is reported. They have been obtained following a four-step strategy. In vitro cytotoxicity of these compounds has been evaluated against four human tumor cell lines (A549, MCF-7, LoVo, and LoVo/DX). Additionally, the mode of binding of the synthesized compounds was evaluated in silico using molecular docking to a 3D structure of β-tubulin based on crystallographic data from the Protein Data Bank and homology methodology. Binding free energy estimates, binding poses, and MlogP values of the compounds were obtained. All triple-modified colchicine derivatives were shown to be active at nanomolar concentrations against three of the investigated cancer cell lines (A549, MCF-7, LoVo). Four of them also showed higher potency against tumor cells over normal cells as confirmed by their high selectivity index values. A vast majority of the synthesized derivatives exhibited several times higher cytotoxicity than colchicine, doxorubicin, and cisplatin.

scholarly journals Synthesis of Some Polysubstituted Nicotinonitriles and Derived Pyrido[2,3-d]pyrimidines asIn VitroCytotoxic and Antimicrobial Candidates

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Hassan M. Faidallah ◽  
Sherif A. F. Rostom ◽  
Khalid A. Khan
Keyword(s):  
Cell Line ◽  
Colon Carcinoma ◽  
Human Tumor ◽  
Human Colon ◽  
Pyrimidine Ring ◽  
Inhibitory Effect ◽  
Breast Adenocarcinoma ◽  
Human Tumor Cell Lines ◽  
E Coli

The synthesis of polysubstituted pyridines, in addition to some derived pyrido[2,3-d]pyrimidine ring systems supported with chemotherapeutically active functionalities, is described. They were evaluated for theirin vitrocytotoxic effects against three different human tumor cell lines (human colon carcinoma HT29, hepatocellular carcinoma Hep-G2, and Caucasian breast adenocarcinoma MCF7). Nine compounds displayed variable cytotoxic potential, among which alkylthio analogs33,34, and37emerged as the most active members, being almost twice as active as doxorubicin against the colon carcinoma HT29 cell line. In addition, the same three analogs showed a clear differential cytotoxic profile as they exhibited a marginal inhibitory effect on the growth of the normal nontransformed human foreskin fibroblast Hs27 cell line. Meanwhile, nineteen compounds were able to exhibit significant antibacterial activity against both Gram-positive and Gram-negative bacteria, together with moderate antifungal activities. The pyrido[2,3-d]pyrimidine-2(1H)-thione30together with its alkylthio derivatives33and34stemmed as the most active antimicrobial members being equipotent to ampicillin againstS. aureus,E. coli,andP. aeruginosa,together with a noticeable antifungal activity againstC. albicans.Compounds33and34could be considered as a promising template for possible dual antimicrobial-anticancer candidates.

scholarly journals Synthesis, Characterization, Antimicrobial and Anticancer Activity of New Bidentate Schiff Base Ligand and their Transition Metal(II) Complexes

2021 ◽  
Vol 33 (7) ◽  
pp. 1488-1494
Author(s):  
S. Arulmozhi ◽  
G. Sasikumar ◽  
A. Subramani ◽  
A. Sudha ◽  
S.J. Askar Ali
Keyword(s):  
Schiff Base ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Schiff Base Ligand ◽  
Pathogenic Bacteria ◽  
Human Tumor ◽  
Spectral Studies ◽  
Breast Adenocarcinoma ◽  
Human Colon Cancer

The metal(II) complexes were synthesized by addition of corresponding MCl2 (M = Mn2+, Ni2+, Cu2+ and Zn2+) with 1,2-bis(1H-pyrrol-2-ylmethylene)diazane in methanol. The ligand acts as a bidentate as confirmed from the mass, IR, UV, NMR and EPR spectral studies. The Schiff base ligand forms hexa-coordinated complexes having octahedral geometry for Mn(II), Ni(II), Zn(II) and Cu(II) complexes. The metal complexes showed an excellent antimicrobial activity spectrum in vitro against both Gram-negative (Klebsiella pneumoniae and Acinetobacter baumannii), Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and human pathogenic bacteria isolates. To find the binding affinity with protein BSA kinase, for that molecular docking studies were also carried for all the four synthesized metal(II) complexes. The anticancer activity of the synthesized metal(II) complexes was also screened against the three human tumor cell lines MCF7 human breast adenocarcinoma cell line, CaSki human caucasian cervical epidermoid carcinoma and HCT116 human colon cancer cell lines. The present study showed that Zn(II) complex showed potent inhibition by the ratio of 80% as compared to the inhibition in the normal cells (L-6).

Synthesis, Characterization and Antitumor Activity of 4-Ferrocenylpyridine-3, 5-Dicarbonitrile Derivatives and Sodium Polymeric Complexes Containing Carbanionic Ligands

2015 ◽  
Vol 1766 ◽  
pp. 9-17
Author(s):  
E. Klimova ◽  
J. Sánchez ◽  
M. Flores ◽  
S. Cortez ◽  
T. Ramírez ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Human Tumor ◽  
X Ray Diffraction ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Biological Specificity ◽  
Polymeric Complexes ◽  
Mcf 7

ABSTRACTThe reactions of 2-cyano-3-ferrocenylacrylonitrile with malononitrile in a ROH/H2O medium in the presence of Na2CO3 afforded 6-alkoxy-2-amino-4-ferrocenylpyridine-3,5-dicarbonitriles, 6-alkoxy-2-amino-4-ferrocenyl-3-ferrocenyl-methyl-3,4-dihydropyridine-3,5-dicarbonitriles and Na+ polymeric complexes: {[Na+(2-ferrocenyl(tetracyano)propenyl)−L]∞ and [Na+(2-amino-3,5-dicyano-4-ferrocenyl-6-pyridyl-dicyanomethyl)−L]∞ where L = ethanol, methanol. Complexes with L = acetonitrile (c), dimethylformamide (d), acetone (e), ethyl acetate (f) were prepared by recrystallization. The structures of the compounds 4b and Na+ polymeric complexes 5c and 6d, e were established by the spectroscopic data and X-ray diffraction analysis. Two compounds 3a and 4a were tested in vitro against six human tumor cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1 to assess their in vitro antitumor activity. The results suggest biological specificity towards PC-3, K-562 and HCT-15 cells for compound 3a, and towards PC-3 cell for compound 4a at doses 50 μM, which are lower than Cisplatin IC50′s in the three cell lines.

scholarly journals Synthesis, Crystal Structure, and Biological Activity ofcis/transAmide Rotomers of (Z)-N′-(2-Oxoindolin-3-ylidene)formohydrazide

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Hatem A. Abdel-Aziz ◽  
Hazem A. Ghabbour ◽  
Wagdy M. Eldehna ◽  
Maha M. Qabeel ◽  
Hoong-Kun Fun
Keyword(s):  
Crystal Structure ◽  
Human Tumor ◽  
Cancer Cell Line ◽  
Monoclinic Space Group ◽  
Moderate Activity ◽  
Standard Drug ◽  
X Ray ◽  
H Nmr ◽  
Mcf 7

(Z)-N′-(2-Oxoindolin-3-ylidene)formohydrazide (2) was synthesized by the reaction of (Z)-3-hydrazonoindolin-2-one (1) with formic acid under reflux. The structure of2was characterized by IR, Mass,1H NMR, and X-ray crystal structure determination. Interestingly, compound2appeared in DMSO-d6ascisandtransamide rotomers in 25% and 75%, respectively. The X-ray analysis showed theZgeometrical isomer of2around –C=N– forcisandtransamide rotomers. The crystal of2belongs to monoclinic, space groupP21/c, witha=4.5206(1) Å,b=22.4747(7) Å,c=17.3637(5) Å,β=103.752(1)°,Z=8,V=1713.57(8) Å3,Dc=1.467 Mg m−3,μ=0.11 mm−1,F(000)=784,R=0.047, andwR=0.123for 3798 observed reflections withI>2σ(I). Compound2exhibited a moderate activity in its antimicrobial evaluation againstE. coliandP. aeruginosaand a good activity againstS. aureusclose to that of the standard drug ciprofloxacin. Thein vitroanticancer activity of2was evaluated against two human tumor cell lines, namely, HepG2 hepatocellular carcinoma and MCF-7 breast cancer. HepG2 cancer cell line was more susceptible to compound2than MCF-7.

scholarly journals In VitroGrowth Inhibitory Activities of Natural Products from Irciniid Sponges against Cancer Cells: A Comparative Study

2016 ◽  
Vol 2016 ◽  
pp. 1-6
Author(s):  
Yosr BenRedjem Romdhane ◽  
Monia Elbour ◽  
Marianna Carbone ◽  
Maria Letizia Ciavatta ◽  
Margherita Gavagnin ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antimicrobial Properties ◽  
Human Tumor ◽  
Cancer Cell Lines ◽  
Marine Sponges ◽  
Inhibitory Effects ◽  
Experimental Conditions ◽  
Growth Inhibitory

Marine sponges of the Irciniidae family contain both bioactive furanosesterterpene tetronic acids (FTAs) and prenylated hydroquinones (PHQs). Both classes of compounds are known for their anti-inflammatory, antioxidant, and antimicrobial properties and known to display growth inhibitory effects against various human tumor cell lines. However, the different experimental conditions of the reportedin vitrobioassays, carried out on different cancer cell lines within separate studies, prevent realistic actual discrimination between the two classes of compounds from being carried out in terms of growth inhibitory effects. In the present work, a chemical investigation of irciniid sponges from Tunisian coasts led to the purification of three known FTAs and three known PHQs. Thein vitrogrowth inhibitory properties of the six purified compounds have been evaluated in the same experiment in a panel of five human and one murine cancer cell lines displaying various levels of sensitivity to proapoptotic stimuli. Surprisingly, FTAs and PHQs elicited distinct profiles of growth inhibitory-responses, differing by one to two orders of magnitude in favor of the PHQs in all cell lines. The obtained comparative results are discussed in the light of a better selection of drug candidates from natural sources.

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