Antitumor Activity (antitumor + activity)

Distribution by Scientific Domains
Distribution within Medical Sciences

Kinds of Antitumor Activity

  • potent antitumor activity
  • significant antitumor activity
  • strong antitumor activity
  • vitro antitumor activity
  • vivo antitumor activity


  • Selected Abstracts


    Design and Synthesis of a Gossypol Derivative with Improved Antitumor Activities

    ARCHIV DER PHARMAZIE, Issue 4 2009
    Yonghua Zhan
    Abstract A novel chemical process has been devised for the synthesis of a new derivative of gossypol, 6,7,6,,7,-tetrahydroxy-5,5,-diisopropyl-3,3,-dimethyl-[2,2']binaphthalenyl-1,4,1,,4,-tetraone (Apogossypolone). This new process has only four steps, with a shorter synthesis span, a simple purification process, and improved yield and quality. The structure of apogossypolone was characterized by 1H-nuclear magnetic resonance, 13C-nuclear magnetic resonance, mass spectroscopy, infrared spectroscopy, and elemental analysis. Cell-cytotoxicity assay demonstrates that apogossypolone is three- to six-fold more potent than the parent compound, (,)-gossypol, in inhibiting the human prostate tumor cell lines PC-3 and DU-145 as well as the human breast cancer cell line MDA-MB-231. The colony-formation assay with DU-145 cells showed that apogossypolone inhibited more than 70% of colony formation at 1 ,M, whereas (,)-gossypol at 10 ,M only inhibited less than 50% of colony formation. The results indicate that apogossypolone exerts strong antitumor activities in human prostate and breast cancer cells, and thus represents a promising cancer therapeutic. [source]


    Synthesis and In-Vitro Antitumor Activities of Some Mannich Bases of 9-Alkyl-1,2,3,4-tetrahydrocarbazole-1-ones

    ARCHIV DER PHARMAZIE, Issue 3 2009
    Jing Chen
    Abstract A novel series of 2-substituted aminomethyl-9-alkyl-1,2,3,4-tetrahydrocarbazole-1-ones 5a,q was synthesized via aminomethylation of 9-alkyl-1,2,3,4-tetrahydrocarbazole-1-ones 4a,e with hydrochlorides of the respective amines 6a,m. The structures of these newly synthesized compounds were characterized by 1H-NMR, MS, and elemental analysis. All the compounds were tested for their cytotoxic activity in vitro against four human tumor cell lines including human non-small lung cancer cells (A549), human gastric adenocarcinoma (SGC), human colon cancer cell (HCT116), human myeoloid leukemia cells (K562), and one multi-drug resistant subline (KB-VCR). Most compounds showed moderate to potent cytotoxic activity against the tested cell lines. Preliminary mechanism research indicated that the most promising compound, 2-diethylaminomethyl-9-methyl-1,2,3,4-tetrahydrocarbazole-1-one 5c, exhibited a potential inhibitory effect against microtubule. [source]


    ChemInform Abstract: Synthesis and in vitro Antitumor Activities of Novel 4-Anilinoquinazoline Derivatives.

    CHEMINFORM, Issue 43 2009
    Venkateshappa Chandregowda
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    ChemInform Abstract: Synthesis, Characterization and anti-HIV and Antitumor Activities of New Coumarin Derivatives.

    CHEMINFORM, Issue 14 2008
    Yaseen A. Al-Soud
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    Novel Skeleton Terpenes from Celastrus hypoleucus with Antitumor Activities.

    CHEMINFORM, Issue 29 2006
    Kui-wu Wang
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]


    ChemInform Abstract: Synthesis, Antifolate, and Antitumor Activities of Classical and Nonclassical 2-Amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.

    CHEMINFORM, Issue 38 2001
    Alleem Gangjee
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    Synthesis of Highly Functionalized Anthraquinones and Evaluation of Their Antitumor Activity,

    EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 27 2007
    Lutz F. Tietze
    Abstract Highly functionalized anthraquinones which derive from the natural products mensacarcin, islandicin, and chrysophanol have been efficiently synthesized using a Diels,Alder reaction as key step. The introduction of the proposed pharmacophoric side chain unit has been achieved by an addition of an aryllithium species onto different aldehydes. Furthermore, the antitumor activity of these novel compounds has been studied by the in vitro growth inhibition of human lung carcinoma cells of line A549.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007) [source]


    Facile Synthesis and In-Vitro Antitumor Activity of Some Pyrazolo[3,4- b]pyridines and Pyrazolo[1,5- a]pyrimidines Linked to a Thiazolo[3,2- a]benzimidazole Moiety

    ARCHIV DER PHARMAZIE, Issue 1 2010
    Hatem A. Abdel-Aziz
    Abstract The key precursor E -3-(N,N -dimethylamino)-1-(3-methylthiazolo[3,2- a]benzimidazol-2-yl)prop-2-en-1-one 4 was synthesized in good yield using Gold's reagent. The reaction of enaminone 4 with 5-amino-3-aryl-1 - phenylpyrazoles 5a, b in refluxing acetic acid in the presence of sulphuric acid, yielded pyrazolo[3,4- b]pyridines 7a, b. Similarly, pyrazolo[1,5- a]pyrimidines 10a, b and 14a,f were prepared by reaction of enaminone 4 with 5-amino-1H -pyrazoles 8a, b and 12a,f, respectively. The structure of pyrazolo[1,5- a]pyrimidine 10b was determined by X-ray diffraction. The synthesized compounds were tested for their in-vitro antitumor activity against the colon cancer cell line CaCo-2; their cytotoxicity against the normal fibroblast cell line BHK was explored as well. Some of the tested compounds exhibited cell growth inhibitory activity. The significant antitumor activity of compound 14f against the CaCo-2 cell line (IC50 = 0.5 ,g/mL) was coupled with a lower toxicity against BHK (IC50 = 2.3 ,g/mL). [source]


    Elucidation of Oxygenation Steps during Oviedomycin Biosynthesis and Generation of Derivatives with Increased Antitumor Activity

    CHEMBIOCHEM, Issue 2 2009
    Felipe Lombó Dr.
    Abstract Eight different angucyclinones have been produced in Streptomyces albus by combining three oxygenase genes together with the polyketide synthase and cyclases genes from the oviedomycin biosynthetic gene cluster from Streptomyces antibioticus ATCC 11891. Four of these compounds were fully characterized for the first time. Three of these angucyclinones,prejadomycin-2-carboxylate (2), 4a,12b-dehydro-UWM6 (5), and prejadomycin (3),show a significant increase in their in vitro antitumor activity relative to oviedomycin (1). A hypothesis for the sequence of tailoring events catalyzed by these three oxygenases during oviedomycin biosynthesis is proposed. In this hypothesis OvmOII acts as a bifunctional oxygenase/dehydratase. [source]


    Design, Synthesis, Docking and Antitumor Activity of Quinazolino [3, 4-a] thieno [3, 2-d] pyrimidin-8-one Derivatives

    CHEMICAL BIOLOGY & DRUG DESIGN, Issue 3 2010
    Youguang Zheng
    Several novel quinazolino [3, 4-a] thieno [3, 2-d] pyrimidin-8-one derivatives were synthesized. All of the compounds were determined against MiaPaCa2 and DU145 cells in vitro, and the crystal structures of analog 8 and 20 in the active site of the EGFR complexes were presented. The entire compounds had been identified by 1HNMR, 13CNMR, IR, MS and EA. [source]


    Synthesis and Antitumor Activity of Novel Dibutyltin Carboxylates of Aminoglucosyl Derivatives

    CHEMICAL BIOLOGY & DRUG DESIGN, Issue 6 2009
    Wei Li
    In this study, di-n-butyltin(IV) oxide was reacted with the amino glucose analog, cis -4-[N -(1,,3,,4,,6,-tetra- O -benzoyl-2-deoxy-glucopyranosyl)imido]-4-oxo-2-butenoic acid (1a) and o -[N -(1,,3,,4,,6,-tetra- O -benzoyl-2-deoxy-glucopyranosyl) carbamoyl] benzoic acid (2a) to give the complexes bis-{cis -4-[N -(1,,3,,4,,6,-tetra- O -benzoyl-2-deoxy-glucopyranosyl)imido-4-oxo-2-butenoic acid]-di-n-butyltin} carboxylate (1) and bis-{o -[N -(1,,3,,4,,6,-tetra- O -benzoyl-2-deoxy-glucopyranosyl) carbamoyl-benzoic acid]-di-n-butyltin}carboxylate (2). These two compounds were then characterized by IR, NMR and MS. In vitro tests showed that both compounds have high cytotoxicity in four tumor cell lines (P388, HL-60, A549 and BEL-7402). Clonogenic assays demonstrated that both compounds 1 and 2 have hematopoietic cell toxicity at 10,6 m. [source]


    ChemInform Abstract: Synthesis of Some New Pyrazole and Pyrimidine Derivatives Carrying a Sulfonamide Moiety of Expected Antitumor Activity and Study of the Synergistic Effect of ,-Irradiation.

    CHEMINFORM, Issue 33 2010
    Mostafa M. Ghorab
    Abstract Several of the new pyrazole and pyrimidine derivatives, e.g. (IIa), (V), (VII), (IX), (XIIa) and (XIVb), are equipotent or even more potent than doxorubicin. [source]


    ChemInform Abstract: Synthesis, Chiral Resolution, and Determination of Novel Furan Lignan Derivatives with Potent Antitumor Activity.

    CHEMINFORM, Issue 30 2010
    Hai Ling Sun
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    ChemInform Abstract: Synthesis and Antitumor Activity of 1-Mesityl-3-(2-naphthoylmethano)-1H-imidazolium Bromide.

    CHEMINFORM, Issue 30 2010
    Xianghui Zeng
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    ChemInform Abstract: Design, Synthesis, Antitumor Activity and Mode of Action of Novel Oxiranyl and Thiiranyl Phenol Derivatives.

    CHEMINFORM, Issue 49 2009
    Zunhua Yang
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    ChemInform Abstract: Synthesis and in vitro Antitumor Activity of New Quinoxaline Derivatives.

    CHEMINFORM, Issue 31 2009
    Paola Corona
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    ChemInform Abstract: Synthesis of ,-Hydroxybutenolides Applying Crossed Aldol Condensation in the Presence of a Bulky Lewis Acid and Their Antitumor Activity.

    CHEMINFORM, Issue 6 2008
    Yumiko Yamano
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    Synthesis and in vitro Antitumor Activity of a New Series of 4-Chloro-2-mercapto-5-methylbenzenesulfonamide Derivatives.

    CHEMINFORM, Issue 52 2007
    J. Slawinski
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]


    Synthesis, Antiviral and Antitumor Activity of 2-Substituted-5-amidino-benzimidazoles.

    CHEMINFORM, Issue 42 2007
    Kristina Starcevic
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]


    Synthesis of the New pseudo-Symmetrical Tamoxifen Derivatives and Their Antitumor Activity.

    CHEMINFORM, Issue 36 2007
    Isamu Shiina
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]


    Synthesis of 1,2,3,4,5,6,7,10-Octahydro-1,5-imino-7,10-dioxo-3-benzazocine-4-carbonit rile Derivative and Evaluation of Antitumor Activity Related to Saframycin and Renieramycin Isoquinolinequinones.

    CHEMINFORM, Issue 22 2007
    Yu-ichi Koizumi
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]


    Synthesis, X-Ray Crystallographic Analysis and Antitumor Activity of 3,6-Bis(substitutedphenyl)-1,4-bis (substitutedphenylsulfonyl)-1,4-dihydro-1,2,4,5-tetrazine.

    CHEMINFORM, Issue 40 2006
    Wei-Xiao Hu
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]


    Synthesis and Antitumor Activity of 2-Aryl-7-fluoro-6-(4-methyl-1-piperazinyl)-4(3H)-quinazolinones.

    CHEMINFORM, Issue 2 2006
    Raid J. Abdel-Jalil
    Abstract For Abstract see ChemInform Abstract in Full Text. [source]


    Synthesis and Antitumor Activity of N,N,-Bis(substitutedphenyl) -3,6-dialkyl-1,4-dihydro-s-tetrazine-1,4-dicarboxamide.

    CHEMINFORM, Issue 36 2005
    Weixiao Hu
    Abstract For Abstract see ChemInform Abstract in Full Text. [source]


    Synthesis and in vitro Antitumor Activity of Substituted Anthracene-1,4-diones.

    CHEMINFORM, Issue 8 2005
    Duy H. Hua
    Abstract For Abstract see ChemInform Abstract in Full Text. [source]


    Synthesis and Antitumor Activity of New Steroidal Nuclear Analogues of Aragusterol A.

    CHEMINFORM, Issue 45 2003
    Hidemichi Mitome
    Abstract For Abstract see ChemInform Abstract in Full Text. [source]


    Two New Sesquiterpenes from the Chinese Herb Halenia elliptica and Their Antibacterial and Antitumor Activity.

    CHEMINFORM, Issue 7 2003
    Jingqiu Dai
    Abstract For Abstract see ChemInform Abstract in Full Text. [source]


    Synthesis, DNA-Inhibiting and Antitumor Activity of Thiosemicarbazones of 2-Formyl-2,5-dimethoxy-2,3-dihydro-4H-pyran, Its Ethyl Analogue and Copper Complex.

    CHEMINFORM, Issue 3 2003
    N. A. Keiko
    No abstract is available for this article. [source]


    ChemInform Abstract: Aziridinyl Quinone Antitumor Agents Based on Indoles and Cyclopent[b]indoles: Structure,Activity Relationships for Cytotoxicity and Antitumor Activity.

    CHEMINFORM, Issue 8 2002
    Edward B. Skibo
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    ChemInform Abstract: Synthesis and Antitumor Activity of Trimethylsilylpropyl Substituted Benzimidazoles.

    CHEMINFORM, Issue 1 2002
    Edmunds Lukevics
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]