cytotoxicity screening of some 3-substituted-4-oxo-imidazolidin-2-(1H)-thione derivatives as anticancer drug.

This study aimed to investigate the antitumor activity of new series of 2-thiohydanotin derivatives ( and ) against two cancer cell lines. A new series of 2-thioxoimidazolidine derivatives () were synthesized and investigated for its structure through spectral analysis and also tested against (HepG-2) and (HCT-116) cell line. Among the synthesized compounds, compound halted liver cancer cells at the G0/G1 phase and triggered apoptosis of liver cancer.

anti-breast cancer study of hybrid cinnamic acid derivatives bearing 2-thiohydantoin moiety.

: To synthesize new hybrid cinnamic acids (, and ) and ester derivatives (, and ) and investigate their anti-breast cancer activities. Compounds were evaluated () for their cytotoxic activities against the MCF-7 cell line. A flow cytometry examination was performed.

cytotoxic investigation of some synthesized 1,6-disubstituted-1-azacoumarin derivatives as anticancer agents.

In this study, novel synthesized 1,6-disubstituted-1-azacoumarin-3-carboxylic acid derivatives were designed, synthesized and evaluated as potential anticancer agents. The cytotoxicity of novel 1-azacoumarin-3-carboxylic acid derivatives was tested using an MTT assay. High potency was shown by DNA flow cytometry on MCF-7 cells for compound .

Design, Synthesis, Cytotoxic Screening and Molecular Docking Studies of Novel Hybrid Thiosemicarbazone Derivatives as Anticancer Agents.

Thiosemicarbazones have been the focus of scientists owing to their broad clinical anticancer range. Herein, A Series of new thiosemicarbazone derivatives 5-9 were synthesized and confirmed through the use of different spectroscopic techniques along with elemental analysis. The in vitro cytotoxic activity of compounds 5-9 against MCF-7 and A549 cell lines and normal breast cells were assessed.

In vivo biological evaluation of sodium salt of ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-yl)-3-(4-hydroxyphenyl) acrylate as anticancer agent.

Nowadays, quinoline scaffold is among the most vital construction compounds for the development of new drugs. The purpose of this research is to evaluate the anti-cancer activity of sodium salt of ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-yl)-3-(4-hydroxyphenyl) acrylate against Ehrlich ascites carcinoma (EAC) cells residing in female mice's peritoneal cavity. The docking study exhibited a favourable interaction between the compound and the receptors 1MOY and 3KJF of osteopontin and caspase 3, respectively.

New Mononuclear and Binuclear Cu(II), Co(II), Ni(II), and Zn(II) Thiosemicarbazone Complexes with Potential Biological Activity: Antimicrobial and Molecular Docking Study.

Herein, we report the synthesis of eight new mononuclear and binuclear Co, Ni, Cu, and Zn methoxy thiosemicarbazone (MTSC) complexes aiming at obtaining thiosemicarbazone complex with potent biological activity. The structure of the MTSC ligand and its metal complexes was fully characterized by elemental analysis, spectroscopic techniques (NMR, FTIR, UV-Vis), molar conductivity, thermogravimetric analysis (TG), and thermal differential analysis (DrTGA). The spectral and analytical data revealed that the obtained thiosemicarbazone-metal complexes have octahedral geometry around the metal center, except for the Zn-thiosemicarbazone complexes, which showed a tetrahedral geometry.

In Vitro Anticancer Evaluation of Some Synthesized 2H-Quinolinone and Halogenated 2H-Quinolinone Derivatives as Therapeutic Agents.

Background: Searching for new cytotoxic agents with apoptosis induction may represent a viable strategy for cancer treatment to overcome the increased resistance to available anticancer agents.

Objective: The purpose of the current study was aimed at preparation and anticancer evaluation of two new series of 2H-quinolinone and halogenated 2H-quinolinone derivatives against two cancer cell lines.

Methods: Two new series of 2H-quinolinone and halogenated 2H-quinolinone derivatives were prepared and screened for their cytotoxicity against breast MCF-7 and liver HepG-2 cancer cell lines as well as normal breast MCF-10a.

In Vivo Biological Evaluation of Ethyl 4-(7-hydroxy-4-methyl-2-oxoquinolin-1- ylamino)-coumarin-3-carboxylate as an Antitumor Agent.

Background: Hybridization of coumarin moiety with additional antitumor pharmacophores is an auspicious stratagem to afford precious therapeutic interference for the medication of cancer.

Objective: The present study aimed to evaluate the antitumor activity of ethyl 4-(7-hydroxy-4-methyl-2- oxoquinolin-1-ylamino)-coumarin-3-carboxylate against Ehrlich Ascites Carcinoma (EAC) cells in the peritoneal cavity of female mice.

Methodology: Molecular docking was used to predict the binding between the test compound and the receptor of breast cancer mutant 3HB5-oxidoreductase, as well as the viability of tumor cells and life span prolongation.

In Vitro Antitumor Evaluation of Some Hybrid Molecules Containing Coumarin and Quinolinone Moieties.

Background: Hybrid molecules furnished by merging two or more pharmacophores is an emerging concept in the field of medicinal chemistry and drug discovery. Currently, coumarin hybrids have attracted the keen attention of researchers to discover their therapeutic capability against cancer.

Objective: The present study aimed to evaluate the in vitro antitumor activity of a new series of hybrid molecules containing coumarin and quinolinone moieties 4 and 5 against four cancer cell lines.

A new class of diamide scaffold: Design, synthesis and biological evaluation as potent antimitotic agents, tubulin polymerization inhibition and apoptosis inducing activity studies.

A new series of diamide functional compounds has been designed, synthesized and confirmed by spectroscopic methods and elemental analyses. All the synthesized compounds were evaluated for their antiproliferative activity on HepG2 cell line. Compounds 3k and 3l were proved to have potent anticancer activity equipotent or more potent than reference compound Combretastatin A-4.

Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.

Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show a potent inhibitory activity of cell proliferation and cell cycle arrest at G/M phase.

Inflammatory Biomarkers of Cardiometabolic Risk in Obese Egyptian Type 2 Diabetics.

Inflammatory biomarkers provide a minimally invasive means for early detection and specific treatment of metabolic syndrome and related disorders. The objective of this work was to search for inflammatory biomarkers of cardiometabolic risk in obese type 2 diabetics. The study was performed on 165 persons attending the medical outpatient clinic of Ismailia General Hospital.

Cyclooxygenase-2 single-nucleotide polymorphisms and hepatocellular carcinoma in Egypt.

Unlabelled: Hepatocellular carcinoma (HCC) is a worldwide neoplasm for which early diagnosis is difficult and the prognosis is usually poor. Overexpression of cyclooxygenase 2 (COX-2) has been suggested to be associated with hepatocarcinogenesis. Although several COX-2 inhibitors have been used in hepatoma therapy, the genetic background between COX-2 and HCC remains largely unknown.

Experimental and spectroscopic studies of charge transfer reaction between sulfasalazine antibiotic drug with different types of acceptors.

The charge-transfer (CT) interactions between the electron donor sulfasalazine (SS) and the acceptors 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), p-chloranil (CHL), picric acid (PA) and iodine have been studied spectrophotometrically in CHCl(3) or CH(3) OH solutions. The formed solid CT complexes were also isolated and characterized through infrared, (1) H-NMR, mass spectra as well as elemental and thermal analysis. The CT complexes were discussed in terms of formation constant (K(CT) ), molar extinction coefficient (ε(CT) ), standard free energy (ΔG°), oscillator strength (f), transition dipole moment (µ), resonance energy (R(N) ) and ionization potential (I(D) ).

Spectroscopic characterizations and biological studies on newly synthesized Cu(2+) and Zn(2+) complexes of first and second generation dendrimers.

The novel Cu(II) and Zn(II) complexes of first and second generation poly(propylene amine) dendrimers (PPA), comprising 1,8-naphthalimde units on periphery have been synthesized. These new complexes were characterized by elemental analysis, molar conductivity, spectral methods (IR, (1)H NMR and UV-vis spectra) and thermal analysis (TG and DTG) techniques. From elemental analysis as well as thermal studies it has found that the first generation dendrimer behaves as bidentate ligand and forming chelates with 1:2 (ligand:metal) and 1:4 (ligand:metal) stoichiometry for second generation dendrimer.

Synthesis and spectroscopic studies of some transition metal complexes of a novel Schiff base ligands derived from 5-phenylazo-salicyladehyde and o-amino benzoic acid.

Cu(II), Mn(II), Ni(II), and Zn(II) metal complexes with novel heterocyclic Schiff base derived from 5-phenyl azo-salicyladehyde and o-amino benzoic acid have been synthesized and characterized on the basis of elemental analyses, electronic, IR, and (1)H NMR spectra, and also by aid of scanning electron microscopy (SEM), X-ray powder diffraction, molar ratio measurements, molar conductivity measurements, and thermogravimetric analyses. It has been found that the Schiff base behaves as neutral tridentate (ONO) ligand forming chelates with 1:1 (metal:ligand) stoichiometry.