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In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
Mahmoodi M,Rajabalian S,Foroumadi A,Hidarykeshel S
Tehran University Medical Journal , 2009,
Abstract: "n Normal 0 false false false EN-US X-NONE AR-SA MicrosoftInternetExplorer4 /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin:0in; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:Arial; mso-bidi-theme-font:minor-bidi;} Background: 4-Aryl-4H-chromenes are novel anticancer agents which induce apoptosis in cancer cells. These compounds were found to induce apoptosis by targeting the tubulin/microtubule system in cell proliferation process. The aim of this study was to report cyototoxic and apoptosis inducing activities of a new series of synthesized 4-aryl-4H-chromenes compounds."n"n Methods: The in vitro cytotoxic activity of the synthesized 4-aryl-4H-chromenes was investigated against a paned of human cancer cell lines including MCF-7 (breast carcinoma), A549 (lung carcinoma), HEPG-2 (liver carcinoma), SW-480 (colon adenocarcinoma), U87-MG (glioblastoma), 1321N1 (astrocytoma), and DAOY (medulloblastoma). The percentage of growth inhibitory activity was evaluated using MTT colorimetric assay versus controls not treated with test derivatives. The data for etoposide, a well known anticancer drug, was included for comparison. For each compound, the 50% inhibitory concentration (IC50) were determined. Apoptosis inducing activity were assessed by DAPI staining."n"n Results: Preliminary screening showed that those chromenes analogs bearing phenyl-isoxazole-3-yl substitution or the derivatives containing methoxyphenyl in chromene ring exhibited cytotoxic and apoptotic inducing activity comparable with or even superior than the reference drug, etoposide. The compounds without this type of substitution have lower activity. "n"nConclusions: Replacement of 3, 4, 5-trimethoxyphenyl group with thiazol ring in the synthesized derivatives reduced the cytotoxic activity. However, the derivatives with phenyl-isoxazole analogue showed potent cytotoxic and apoptotic inducing activity.
New Catechol Derivatives of Safrole and Their Antiproliferative Activity towards Breast Cancer Cells  [PDF]
Alejandro Madrid Villegas,Luis Espinoza Catalán,Iván Montenegro Venegas,Joan Villena García,Héctor Carrasco Altamirano
Molecules , 2011, DOI: 10.3390/molecules16064632
Abstract: Catechols were synthesized from safrole. Nine derivatives were prepared and assessed for antiproliferative effects using different human cell lines. The in vitro growth inhibition assay was based on the sulphorhodamine dye to quantify cell viability. The derivatives 4-allylbenzene-1,2-diol (3), 4 4-[3-(acetyloxy)propyl]-1,2-phenylene diacetate (6) and 4-[3-(acetyloxy)propyl]-5-nitro-1,2-phenylene diacetate (10) showed higher cytotoxicity than the parent compound 2 in tests performed on two breast cancer cell lines (MCF-7 and MDA-MB-231). The IC50 values of 40.2 ± 6.9 μM, 5.9 ± 0.8 μM and 33.8 ± 4.9 μM, respectively, were obtained without toxicity towards dermal human fibroblast (DHF cells).
N-Heterocyclic carbene–palladium catalysts for the direct arylation of pyrrole derivatives with aryl chlorides
Ismail ?zdemir,Nevin Gürbüz,Nazan Kalo?lu,?znur Do?an
Beilstein Journal of Organic Chemistry , 2013, DOI: 10.3762/bjoc.9.35
Abstract: New Pd–NHC complexes have been synthesized and employed for palladium-catalyzed direct arylation of pyrrole derivatives by using electron-deficient aryl chlorides as coupling partners. The desired coupling products were obtained in moderate to good yields by using 1 mol % of these air-stable palladium complexes. This is an advantage compared to the procedures employing air-sensitive phosphines, which have been previously shown to promote the coupling of aryl chlorides with heteroarenes.
New acylides: synthesis of 3-O-[γ-(4-oxo-2-aryl-thiazolidin-3-yl)butyryl]erythromycin A derivatives  [cached]
Deepa Pandey,Wahajul Haq,Seturam B Katti
Beilstein Journal of Organic Chemistry , 2008, DOI: 10.3762/bjoc.4.14
Abstract: In search of new erythromycin derivatives 3-O-[γ-(4-oxo-2-aryl-thiazolidin-3-yl)butyryl]erythromycin A derivatives have been synthesized. The 3-hydroxy group was derivatised to a primary amine and subsequently the thiazolidinone nucleus was generated at the amino functionality through DCC mediated one-pot three-component reaction in good yields.
Synthesis of 2,3-Dioxo-5-(substituted)arylpyrroles and Their 2-Oxo-5-aryl-3-hydrazone Pyrrolidine Derivatives  [PDF]
M. F. Mohammat,Z. Shaameri,A. S. Hamzah
Molecules , 2009, DOI: 10.3390/molecules14010250
Abstract: Some novel2,3-dioxo-5-(substituted)arylpyrroles have been synthesized. Among these, pyrrolidine compound 1b was converted to 2,3-dioxo-5-aryl pyrrolidine 2b. Finally a set of hydrazone derivatives was obtained from the reaction of 2b with various hydrazine salts. The structures of all the new synthesized compounds were confirmed by elemental analyses, IR and 1H-NMR spectra.
Synthesis and Antibacterial Screening of Some 1-Aroyl-3-aryl Thiourea Derivatives  [PDF]
Love Kumar Soni,Tamanna Narsinghani,Rica Jain
ISRN Medicinal Chemistry , 2014, DOI: 10.1155/2014/393102
Abstract: A series of 1-aroyl-3-aryl thioureas derivatives were synthesized and evaluated for antibacterial activity. The results indicated that the compounds possessed higher activity against gram-negative bacteria than gram-positive bacteria. Amongst all these compounds, C18 (89.4%) exhibited the greatest antibacterial activity against gram-negative bacteria while C5 (85.6%) displayed maximum antibacterial activity against gram-positive bacteria. Preliminary study of the structure-activity relationship revealed that an electronic factor on aryl rings had a great effect on the antibacterial activity of these compounds. 1. Introduction The increased use of antibacterial and antifungal agents has resulted in the development of drug resistant microbial pathogens which results in failure in clinical application of these agents. This highlights the incessant need for the development of new classes of antimicrobial agents and alteration of known drugs in such way that would allow them to retain their physiological action but reduce their resistance to the pathogen. Thiourea derivatives are versatile building blocks for the synthesis of a variety of heterocyclic compounds and display a wide spectrum of biological activities such as antimicrobial [1–4], antimalarial [5], antitubercular [6], anticancer [7], anti-HIV [8], carbonic anhydrases inhibitor [9], appetite suppressants [10], β3-adrenergic receptor agonists [11], and CNS activity [12]. Therefore, their beneficial properties have prompted several groups to study these compounds. We have been interested in antimicrobial agents for a few years and have performed QSAR analysis and synthesis of antimicrobial agents [13–15]. Here in the present work we report the synthesis and screening of some 1-aroyl-3-aryl thiourea derivatives for their antimicrobial potency. 2. Experimental Synthesis of some 1-aroyl-3-aryl thioureas (C1–C18) (Figure 1 and Table 1) was carried out by treating substituted benzoyl chloride with an equimolar quantity of potassium thiocyanate in acetone followed by reaction with an equimolar amount of substituted anilines to furnish the 1-aroyl-3-aryl thiourea derivatives. Table 1: Synthesized 1-aroyl-3-aryl thiourea derivatives. Figure 1: Synthesis of 1-aroyl-3-aryl thiourea. 2.1. General Procedure for the Synthesis of 1-Aroyl-3-aryl Thioureas A solution of substituted benzoyl chloride (10?mmol) in acetone (50?mL) was added dropwise to a suspension of potassium thiocyanate (10?mmol) in acetone (30?mL) and the reaction mixture was refluxed for 30?min. After cooling to room temperature, a solution of
Synthesis and antiinflammatory activity of n-aryl anthranilic acid and its derivatives  [cached]
Joshi J,Patel V,Patel K,Rana D
Indian Journal of Pharmaceutical Sciences , 2007,
Abstract: N-aryl anthranilic acid and its derivatives (3a-f) have been synthesized via Ullmann condensation of o-chloro benzoic acid with various substituted anilines (2a-f) in the presence of cupric oxide and anhydrous potassium carbonate. All the synthesized compounds (3a-f) were characterized by mp, TLC, UV, IR, 1 H NMR and mass spectral analysis. All the synthesized compounds (3a-f) were screened for their antiinflammatory activity by carrageenan induced rat paw edema method. All the synthesized compounds (3a-f) showed significant antiinflammatory activity. Compounds 3a and 3c were found to be the most potent compounds.
Synthesis and antimicrobial screening of pyrazolo-3-aryl quinazolin-4(3h)ones  [cached]
Deshmukh M,Patil S,Patil S,Jadhav S
Indian Journal of Pharmaceutical Sciences , 2010,
Abstract: 2-thio-3-aryl quinazolin-4(3H)one (1) was synthesized by reacting anthranilic acid with thiocarbamate salts of substituted aniline and carbon disulphide, which on reflux with excess of hydrazine hydrate to form 2-hydrazino quinazolin-4(3H)one derivatives (2). The reaction of (2) with variously substituted aryl aldehydes gave the corresponding hydrazones (3). Further, the cyclization of compound (3) in acetic anhydride gave tricyclic pyrazoloquinazolinones (4). All newly synthesized compounds have been tested for their antibacterial activity against gram +ve bacteria B. substilis, S. aureus and gram -ve bacteria E. coli, P. vulgaris. The species used for antifungal activity are Aspergillus niger and Phytophora. Introduction of -OCH3, -OH and -Cl groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.
SYNTHESIS OF NINE SAFROLE DERIVATIVES AND THEIR ANTIPROLIFERATIVE ACTIVITY TOWARDS HUMAN CANCER CELLS
ESPINOZA CATALáN,LUIS; MADRID VILLEGAS,ALEJANDRO; TABORGA LIBER,LAUTARO; VILLENA GARCíA,JOAN; CUELLAR FRITIS,MAURICIO; CARRASCO ALTAMIRANO,HéCTOR;
Journal of the Chilean Chemical Society , 2010, DOI: 10.4067/S0717-97072010000200016
Abstract: safrole from sassafras oil (ocoteapretiosa mez., lauraceae), is an abundant natural product showing interesting functionality and chemical structure. starting from safrole, nine derivatives were prepared and assessed for antiproliferative effect using different human cell lines. the in vitro growth inhibition assay was based on the sulphorhodamine dye to quantify cell viability. some safrole derivatives, (2e')-3-(3',4'-methylenedioxi)phenyl acrylaldehyde (3) and 4-allyl-5-nitrobenzene-1,2-diol (4) presented better antiproliferative effect than the parent compound on two breast cancer cell lines (mcf-7 and mda-mb-231) and one human colorectal cancer cell line (dld-1) with ic50 values of 55.0 + 7.11 um, 37.5 +2.65 um and 44.0 + 6.92 μm, respectively, without toxicity towards dermal human fibroblast (dhf cells).
SYNTHESIS OF NINE SAFROLE DERIVATIVES AND THEIR ANTIPROLIFERATIVE ACTIVITY TOWARDS HUMAN CANCER CELLS  [cached]
LUIS ESPINOZA CATALáN,ALEJANDRO MADRID VILLEGAS,LAUTARO TABORGA LIBER,JOAN VILLENA GARCíA
Journal of the Chilean Chemical Society , 2010,
Abstract: Safrole from sassafras oil (Ocoteapretiosa Mez., Lauraceae), is an abundant natural product showing interesting functionality and chemical structure. Starting from safrole, nine derivatives were prepared and assessed for antiproliferative effect using different human cell lines. The in vitro growth inhibition assay was based on the sulphorhodamine dye to quantify cell viability. Some safrole derivatives, (2E')-3-(3',4'-methylenedioxi)phenyl acrylaldehyde (3) and 4-allyl-5-nitrobenzene-1,2-diol (4) presented better antiproliferative effect than the parent compound on two breast cancer cell lines (MCF-7 and MDA-MB-231) and one human colorectal cancer cell line (DLD-1) with IC50 values of 55.0 + 7.11 uM, 37.5 +2.65 uM and 44.0 + 6.92 μM, respectively, without toxicity towards dermal human fibroblast (DHF cells).
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