scholarly journals Facile synthesis, characterization, and cytotoxicity study of new 3-(indol-2-yl)bicyclotetrazatridecahexaens

2017 ◽  
Vol 95 (8) ◽  
pp. 858-862 ◽  
Author(s):  
Kamal Sweidan ◽  
Dima A. Sabbah ◽  
Sanaa Bardaweel ◽  
Ghassan Abu Sheikha ◽  
Tariq Al-Qirim ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Hct116 Cell ◽  
Chloroacetic Acid ◽  
Human Colon ◽  
Cytotoxic Activities ◽  
Human Skin Fibroblast ◽  
Normal Human Skin ◽  
H Nmr ◽  
Elemental Analyses

A new series of thiosemicarbazone-based indole derivatives 12–15 has been prepared by condensation reaction of indole-2-carboxamide derivatives 8–11 with thiosemicarbazide. The former compounds underwent intracyclization in the presence of chloroacetic acid and sodium acetate to afford a set of new 3-(indol-2-yl)bicyclotetrazatridecahexaens 16–19. These newly synthesized compounds have been characterized by means of FTIR, 1H NMR, 13C NMR, and HRMS and by elemental analyses. Cytotoxic activities of the prepared compounds along with LY294002 were evaluated in vitro against normal human skin fibroblast, human colon carcinoma (HCT116), and leukemia (K562) cell lines; results revealed that the series inhibits only HCT116 cell line. In addition, results showed that compound 18 exerts moderate potency in HCT116 with an IC50 value of 54 μmol/L and significantly induces apoptosis.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

scholarly journals Synthesis of Novel 1,2,4-Triazolyl Coumarin Derivatives as Potential Anticancer Agents

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Lamya H. Al-Wahaibi ◽  
Hanaa M. Abu-Melha ◽  
Diaa A. Ibrahim
Keyword(s):  
Colon Cancer ◽  
Molecular Docking ◽  
Anticancer Agents ◽  
Tyrosine Kinases ◽  
Hct116 Cell ◽  
Human Colon ◽  
Docking Studies ◽  
Coumarin Derivatives ◽  
Human Colon Cancer

A series of novel coumarin derivatives carrying 1,2,4-triazole or 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole moieties were prepared and evaluated in vitro as anticancer in the human colon cancer (HCT116) cell line. The derivatives 4c and 8c exhibited marked anticancer activity with IC50 values 4.363 and 2.656 µM, respectively. The molecular docking studies suggested possible interaction with tyrosine kinases (CDK2).

Synthesis and in vitro Biological Activity of New 4,6-Disubstituted 3(2H)-Pyridazinone-acetohydrazide Derivatives

2012 ◽  
Vol 67 (5-6) ◽  
pp. 257-265
Author(s):  
Murat Sukuroglu ◽  
Tijen Onkol ◽  
Fatma Kaynak Onurdağ ◽  
Gulsen Akalın ◽  
M. Fethi Şahin
Keyword(s):  
Biological Activity ◽  
Antimicrobial Activities ◽  
Cytotoxic Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Preliminary Results ◽  
H Nmr ◽  
Pyridazinone Derivatives

New 3(2H)-pyridazinone derivatives containing a N’-benzyliden-acetohydrazide moiety at position 2 were synthesized. The structures of these newly synthesized compounds were confi rmed by IR, 1H NMR, and MS data. These compounds were tested for their antibacterial, antifungal, antimycobacterial, and cytotoxic activities. The compounds 2-[4-(4-chlorophenyl)- 6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-tert-butylbenzyliden)acetohydrazide and 2-[4-(4-chlorophenyl)-6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-chlorobenzyliden) acetohydrazide exhibited activity against both Gram-positive and Gram-negative bacteria. Most of the compounds were active against E. coli ATCC 35218. The preliminary results of this study revealed that some target compounds exhibited promising antimicrobial activities

scholarly journals Synthesis, Characterization, and Interaction with Biomolecules of Platinum(II) Complexes with Shikimic Acid-Based Ligands

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Yan Peng ◽  
Min-Min Zhang ◽  
Zhen-Feng Chen ◽  
Kun Hu ◽  
Yan-Cheng Liu ◽  
...  
Keyword(s):  
Shikimic Acid ◽  
Covalent Binding ◽  
Carbon Chain ◽  
Water Soluble ◽  
Cytotoxic Activities ◽  
Experimental Conditions ◽  
H Nmr ◽  
Mtt Method ◽  
Low Cytotoxicity

Starting from the active ingredient shikimic acid (SA) of traditional Chinese medicine and NH2(CH2)nOH, (n=2–6), we have synthesized a series of new water-soluble Pt(II) complexes PtLa–eCl2, where La–eare chelating diamine ligands with carbon chain covalently attached to SA (La–e= SA-NH(CH2)nNHCH2CH2NH2; La,n=2; Lb,n=3; Lc,n=4; Ld,n=5; Le,n=6). The results of the elemental analysis, LC-MS, capillary electrophoresis, and1H,13C NMR indicated that there was only one product (isomer) formed under the present experimental conditions, in which the coordinate mode of PtLa–eCl2was two-amine bidentate. Theirin vitrocytotoxic activities were evaluated by MTT method, where these compounds only exhibited low cytotoxicity towards BEL7404, which should correlate their low lipophilicity. The interactions of the five Pt(II) complexes with DNA were investigated by agarose gel electrophoresis, which suggests that the Pt(II) complexes could induce DNA alteration. We also studied the interactions of the Pt(II) complexes with5′-GMP with ESI-MS and1H NMR and found that PtLbCl2, PtLcCl2, and PtLdCl2could react with5′-GMP to form mono-GMP and bis-GMP adducts. Furthermore, the cell-cycle analysis revealed that PtLbCl2, PtLcCl2cause cell G2-phase arrest after incubation for 72 h. Overall, these water-soluble Pt(II) complexes interact with DNA mainly through covalent binding, which blocks the DNA synthesis and replication and thus induces cytotoxicity that weakens as the length of carbon chain increases.

scholarly journals Ultrasonication-Induced Synthesis and Antimicrobial Evaluation of Some Multifluorinated Pyrazolone Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Anil Gadhave ◽  
Shashikant Kuchekar ◽  
Bhausaheb Karale
Keyword(s):  
Fungal Pathogens ◽  
Condensation Reaction ◽  
Ultrasound Irradiation ◽  
Conventional Heating ◽  
Aspergillus Clavatus ◽  
H Nmr ◽  
Pyrazolone Derivatives ◽  
Knoevenagel Condensation Reaction ◽  
Antimicrobial Evaluation

A series of novel fluorine containing pyrazole-pyrazolone (4a–j) and chromone-pyrazolone (5a–i) was synthesized from multifluorinated pyrazolone by the Knoevenagel condensation reaction. All compounds were synthesized by conventional heating as well as ultrasound irradiation technique. It was found that ultrasonication method was more efficient than conventional heating method. The newly synthesized compounds were subjected forin vitroantimicrobial screening against four bacterial pathogens, namely,Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli,andPseudomonas aeruginosaand three fungal pathogensCandida albicans, Aspergillus niger,andAspergillus clavatus, using broth microdilution (MIC) method (CLSI guidelines). Among them, some compounds exhibited promising antibacterial activity against the tested strains. All synthesized compounds were characterized by IR,1H-NMR, mass, and elemental analysis.

The Synthesis and Anticancer Activities of Peptide 5-fluorouracil Derivatives

2009 ◽  
Vol 2009 (4) ◽  
pp. 261-264 ◽  
Author(s):  
Xiaowei Yan ◽  
Maolin Hu ◽  
Qian Miao ◽  
Shun Wang ◽  
Kejian Zhao
Keyword(s):  
Cell Lines ◽  
Mass Spectra ◽  
Anticancer Activities ◽  
H Nmr ◽  
Elemental Analyses ◽  
C Nmr

A new series of peptide 5-fluorouracil derivatives was designed and synthesised in order to test in vitro anticancer activities. The results indicated that peptide 5-fluorouracil derivatives possessed anticancer activities against human HL-60 and Bel-7402 cell lines. The structures of the compounds were determined by means of 1H NMR, 13C NMR, IR, mass spectra and elemental analyses.

scholarly journals Nimesulide Based Novel Glycolamide Esters: Their Design, Synthesis, and Pharmacological Evaluation

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kavitha Kankanala ◽  
Vangala Ranga Reddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
Khagga Mukkanti ◽  
...  
Keyword(s):  
Cancer Cell Line ◽  
Human Colon ◽  
Colon Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Step Method ◽  
Human Colon Cancer ◽  
Cytotoxic Effects ◽  
Design Synthesis ◽  
First Time

The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.

Synthesis of three novel imidazolyl-appended porphyrins and their cytostatic and phototoxic activity on A431 cells

2013 ◽  
Vol 17 (11) ◽  
pp. 1113-1119 ◽  
Author(s):  
Guiping Yao ◽  
Zengqi Zhang ◽  
Jun Li ◽  
Xiaoqin Su ◽  
Wanjun Sun ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Singlet Oxygen ◽  
Uv Light ◽  
Cutaneous Squamous Cell Carcinoma ◽  
Anticancer Activities ◽  
A431 Cells ◽  
Selective Cytotoxicity ◽  
H Nmr ◽  
Elemental Analyses

Three imidazolyl-appended porphyrins were synthesized and characterized by 1 H NMR, elemental analyses, MS and UV-vis spectra. Anticancer activities of porphyrins have been evaluated against cutaneous squamous cell carcinoma (A431 cells) in vitro. The results indicate that the porphyrins have high selective cytotoxicity towards A431 cells in the absence of light and improved phototoxic activity upon exposure to UV light. The yield of singlet oxygen generated by porphyrins were also evaluated by measuring the absorption decay of 1,3-diphenylisobenzofuran (DPBF) in DMF. The phototoxicities of porphyrins against A431 cells were enhanced along with the increase of singlet oxygen.

scholarly journals Synthesis and Characterization of New Amino Acid-Schiff Bases and Studies their Effects on the Activity of ACP, PAP and NPA Enzymes (In Vitro)

2012 ◽  
Vol 9 (2) ◽  
pp. 962-969 ◽  
Author(s):  
Zahraa Salim M. Al-Garawi ◽  
Ivan Hameed R. Tomi ◽  
Ali Hussein R. Al-Daraji
Keyword(s):  
Schiff Base ◽  
Condensation Reaction ◽  
Synthesis And Characterization ◽  
Activation Effect ◽  
Inhibition Effect ◽  
H Nmr ◽  
Ft Ir ◽  
High Concentrations

In this study, two new Schiff base compounds derived from the condensation reaction ofL-glycine andL-tryptophan with 4-methylbenzal-dehyde have been synthesized. The Schiff base compounds were characterized by FT-IR, UV and1H NMR spectroscopy. Their effects on the activity of total (ACP), prostatic (PAP) and non prostatic (NPA) acid phosphatase enzymes were studied. The Schiff base derived fromL-glycine (A) demonstrated inhibition effect on the ACP and NPA activities and activation effect on PAP activity. The Schiff base derived fromL-tryptophan (B) demonstrated semi fixed inhibition effects on the ACP and NPA activities at high concentrations (5.5×10-2, 5.5×10-3and 5.5×10-4M) and activator effect at low concentration (5.5×10-5M) while it was exhibits as activator on PAP activity.

scholarly journals New CXCR4 Antagonist Peptide R (Pep R) Improves Standard Therapy in Colorectal Cancer

Cancers ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 1952
Author(s):  
Crescenzo D’Alterio ◽  
Antonella Zannetti ◽  
Anna Maria Trotta ◽  
Caterina Ieranò ◽  
Maria Napolitano ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Colon Cancer ◽  
Cell Growth ◽  
Standard Therapy ◽  
Hct116 Cell ◽  
Human Colon ◽  
Chemotherapeutic Agents ◽  
Cxcr4 Antagonist ◽  
Human Colon Cancer

The chemokine receptor CXCR4 is overexpressed and functional in colorectal cancer. To investigate the role of CXCR4 antagonism in potentiating colon cancer standard therapy, the new peptide CXCR4 antagonist Peptide R (Pep R) was employed. Human colon cancer HCT116 xenograft-bearing mice were treated with chemotherapeutic agents (CT) 5-Fluorouracil (5FU) and oxaliplatin (OX) or 5FU and radio chemotherapy (RT-CT) in the presence of Pep R. After two weeks, CT plus Pep R reduced by 4-fold the relative tumor volume (RTV) as compared to 2- and 1.6-fold reductions induced, respectively, by CT and Pep R. In vitro Pep R addition to CT/RT-CT impaired HCT116 cell growth and further reduced HCT116 and HT29 clonal capability. Thus, the hypothesis that Pep R could target the epithelial mesenchyme transition (EMT) process was evaluated. While CT decreased ECAD and increased ZEB-1 and CD90 expression, the addition of Pep R restored the pretreatment expression. In HCT116 and HT29 cells, CT/RT-CT induced a population of CD133+CXCR4+ cells, supposedly a stem-resistant cancer cell population, while Pep R reduced it. Taken together, the results showed that targeting CXCR4 ameliorates the effect of treatment in colon cancer through inhibition of cell growth and reversal of EMT treatment-induced markers, supporting further clinical studies.

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