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Antitumor Activity (antitumor + activity)
Kinds of Antitumor Activity Selected AbstractsDesign and Synthesis of a Gossypol Derivative with Improved Antitumor ActivitiesARCHIV DER PHARMAZIE, Issue 4 2009Yonghua 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-onesARCHIV DER PHARMAZIE, Issue 3 2009Jing 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 2009Venkateshappa 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 2008Yaseen 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 2006Kui-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 2001Alleem 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 2007Lutz 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 MoietyARCHIV DER PHARMAZIE, Issue 1 2010Hatem 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 ActivityCHEMBIOCHEM, Issue 2 2009Felipe 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 DerivativesCHEMICAL BIOLOGY & DRUG DESIGN, Issue 3 2010Youguang 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 DerivativesCHEMICAL BIOLOGY & DRUG DESIGN, Issue 6 2009Wei 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 2010Mostafa 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 2010Hai 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 2010Xianghui 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 2009Zunhua 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 2009Paola 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 2008Yumiko 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 2007J. 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 2007Kristina 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 2007Isamu 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 2007Yu-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 2006Wei-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 2006Raid 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 2005Weixiao 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 2005Duy 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 2003Hidemichi 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 2003Jingqiu 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 2003N. 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 2002Edward 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 2002Edmunds 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] |