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Samir Messaoudi et al.
Journal of medicinal chemistry, 52(14), 4538-4542 (2009-06-18)
Herein is reported a convergent synthesis of isocombretastatins A, a novel class of potent antitubulin agents. These compounds having a 1,1-diarylethylene scaffold constitute the simplest isomers of natural Z-combretastatins A that are easy to synthesize without need to control the
Elizabeth W Chia et al.
Bioorganic & medicinal chemistry, 16(21), 9432-9442 (2008-10-07)
Sixteen new thiazine-quinoline-quinones have been synthesised, plus one bicyclic analogue. These compounds inhibited neutrophil superoxide production in vitro with IC(50)s as low 60 nM. Compounds with high in vitro anti-inflammatory activity were also tested in a mouse model of acute
Romeo Romagnoli et al.
Journal of medicinal chemistry, 56(6), 2606-2618 (2013-03-01)
Two new series of inhibitors of tubulin polymerization based on the 2-(alkoxycarbonyl)-3-(3',4',5'-trimethoxyanilino)benzo[b]thiophene and thieno[2,3-b]pyridine molecular skeletons were synthesized and evaluated for antiproliferative activity on a panel of cancer cell lines, inhibition of tubulin polymerization, cell cycle effects, and in vivo
Ravi Kumar Anchoori et al.
Journal of medicinal chemistry, 51(19), 5953-5957 (2008-09-10)
Current microtubule inhibitory agents used in the clinic to treat cancer have severe side effects, and development of resistance is frequent. We have evaluated the antitumor effect of a novel 30-compound library of phenoxy pyridine and phenyl sulfanyl pyridine derivatives.
Satoru Itoh et al.
Mutation research. Genetic toxicology and environmental mutagenesis, 782, 18-23 (2015-04-14)
The liver micronucleus test is an important method to detect in vivo genotoxicants, especially those that require metabolic activation for their genotoxicity. We have already reported that structural or numerical chromosome aberration inducers have to be given before or after
A randomized trial of colchicine for acute pericarditis.
Stephen Goldfinger
The New England journal of medicine, 370(8), 780-780 (2014-02-21)
John Ciriello
Brain research bulletin, 116, 81-92 (2015-07-07)
Urocortin-1 (UCN-1), a neuropeptide closely related to the hypothalamic hormone corticotropin-releasing factor, has been associated with stress, feeding behaviors, cardiovascular control, and to exhibit functional gender differences. This study was done to investigate whether estrogen (E; 17β-estradiol) treatment (9 weeks)
Saime Paydas et al.
American journal of therapeutics, 20(4), 344-346 (2012-09-15)
Acute leukemia has been reported as secondary to radiation therapy in patients with ankylosing spondylitis (AS). AA amyloidosis secondary to AS causes progressive organ failure. Although new therapeutic choices can be used, response to therapy in secondary amyloidosis is not
R F Ludueña et al.
Current opinion in cell biology, 4(1), 53-57 (1992-02-01)
In the past year, much has been learned about structure-function correlations in the tubulin molecule, and specifically about the nature and roles of post-translational modifications and tubulin isotypes. The interactions between tubulin and its ligands--both microtubule-associated proteins and anti-mitotic drugs--are
Ruling revives gout drug competition.
Jaimy Lee
Modern healthcare, 45(3), 17-17 (2015-02-13)
Michael Cifuentes et al.
Bioorganic & medicinal chemistry letters, 16(10), 2761-2764 (2006-03-01)
A series of modified colchicine and isocolchicine analogs (C-7 substituent) were synthesized and evaluated in vitro against a PC3 cancer cell line and for inhibition of microtubule polymerization. The colchicine analogs all displayed strong inhibition of tubulin polymerization, while compounds
V Helsen et al.
Acta clinica Belgica, 68(2), 113-115 (2013-08-24)
A 83-year-old woman was admitted to hospital with chest pain, fever, dry cough and palpitations. Chest X-ray revealed a pleural effusion, assumed to be caused by cardiac failure and respiratory infection. Despite treatment with antibiotics and diuretics, the pleural effusion
Umit Zan et al.
Cytotechnology, 63(3), 239-245 (2011-01-22)
Rocuronium bromide (RB), an aminosteroid type neuromuscular blocking agent, acts by reducing or inhibiting the depolarising effect of acetylcholine on the terminal disc of the muscle cell. To our knowledge, there is no adequate information on the genotoxic effects of
Yong Qian et al.
Bioorganic & medicinal chemistry, 18(23), 8218-8225 (2010-11-03)
A series of novel chalcone guanidine derivatives (4a-4q) have been designed and synthesized, and their biological activity were also evaluated as potential antiproliferative and antitubulin polymerization inhibitors. Compound 4q showed the most potent biological activity (IC₅₀ = 0.09 ± 0.01
Colchicine effect on P-glycoprotein expression and activity: in silico and in vitro studies.
Silva R, Carmo H, Vilas-Boas V, et al.
Chemico-Biological Interactions, 218, 50-62 (2014)
Sébastien Preau et al.
Critical care medicine, 41(7), e125-e133 (2013-03-13)
Macrophage migration inhibitory factor (MIF) has been recognized as a potent proinflammatory mediator that may induce myocardial dysfunction. Mechanisms by which MIF affects cardiac function are not completely elucidated; yet, some macrophage migration inhibitory effects have been related to changes
Thomas Strömberg et al.
Medical oncology (Northwood, London, England), 32(7), 188-188 (2015-05-30)
Diffuse large B-cell lymphoma (DLBCL) is the most common lymphoma in adults. Although chemotherapy in combination with anti-CD20 antibodies results in a cure rate of 60-70 %, novel treatment approaches are warranted for the remaining patients. The insulin-like growth factor-1
Alberto Massarotti et al.
ChemMedChem, 7(1), 33-42 (2011-10-13)
Computational approaches have been increasingly applied to drug design over the past three decades and have already provided some useful results in the discovery of anticancer drugs. Given the increased availability of crystal structures in recent years, a growing number
Yan Lu et al.
Pharmaceutical research, 29(11), 2943-2971 (2012-07-21)
Tubulin dynamics is a promising target for new chemotherapeutic agents. The colchicine binding site is one of the most important pockets for potential tubulin polymerization destabilizers. Colchicine binding site inhibitors (CBSI) exert their biological effects by inhibiting tubulin assembly and
Yaqin Zhu et al.
Pharmaceutical research, 31(12), 3289-3303 (2014-05-27)
Using different chain lengths of PEG as linkers to develop a novel folate (FA) and TAT peptide co-modified doxorubicin (DOX)-loaded liposome (FA/TAT-LP-DOX) and evaluate its potential for tumor targeted intracellular drug delivery. FA/TAT-LP-DOX was prepared by pH gradient method and
Vladimir Bogdanov et al.
Basic research in cardiology, 116(1), 63-63 (2021-10-30)
It is widely assumed that synthesis of membrane proteins, particularly in the heart, follows the classical secretory pathway with mRNA translation occurring in perinuclear regions followed by protein trafficking to sites of deployment. However, this view is based on studies
Michael George et al.
Arthritis care & research, 66(8), 1258-1262 (2014-01-01)
American College of Rheumatology and European League Against Rheumatism guidelines recommend colchicine to prevent gout flares in patients initiating and increasing uric acid–lowering therapy until serum uric acid is maintained at ≤6 mg/dl. We aimed to evaluate how well colchicine
Anne Zuse et al.
Journal of medicinal chemistry, 49(26), 7816-7825 (2006-12-22)
A novel series of 9-benzylidene-naphtho[2,3-b]thiophen-4-ones and structurally related compounds were synthesized and evaluated for their ability to inhibit tubulin polymerization. The 4-hydroxy-3,5-dimethoxy-benzylidene analogue 15d was identified as a potent cytotoxic agent in an assay based on K562 leukemia cells. Antiproliferative
Michaela Pojarová et al.
Bioorganic & medicinal chemistry, 15(23), 7368-7379 (2007-09-25)
Cell cycle arrest of malignant cells is an important option for cancer treatment. In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with malononitrile. The resulting methylene propanedinitriles inhibited the growth of MDA-MB 231 and MCF-7 breast
Laura Jung et al.
Molecular human reproduction, 20(6), 538-549 (2014-02-07)
The advent of human induced pluripotent stem cells (hiPSC) is revolutionizing many research fields including cell-replacement therapy, drug screening, physiopathology of specific diseases and more basic research such as embryonic development or diseases modeling. Despite the large number of reports
Yu-Hsiang Lo et al.
Journal of medicinal chemistry, 51(9), 2682-2688 (2008-04-05)
Compounds 2a- h and 6 displayed significant GI 50 values of 10(-7)-10(-6) M against various cancer cell lines. Of these compounds, 2-(6-(2-trifluoromethylphenyl))-3(Z)-hexen-1,5-diynyl)aniline (2c) showed the most potent growth inhibition activity. Compound 2c also arrested cancer cells in the G2/M phase
Pu Hu et al.
Translational psychiatry, 10(1), 396-396 (2020-11-13)
Early-life stress (ELS) leads to stress-related psychopathology in adulthood. Although dysfunction of corticotropin-releasing hormone (CRH) signaling in the bed nucleus of the stria terminalis (BNST) mediates chronic stress-induced maladaptive affective behaviors that are historically associated with mood disorders such as
Jian-Xin Duan et al.
Journal of medicinal chemistry, 50(5), 1001-1006 (2007-02-09)
A series of 3-aroyl indazoles was synthesized. Modification of the C-7 position resulted in a significant structure-activity relationship (SAR) with acetylene modifications conferring unusual potency in a tumor cell cytotoxicity assay. The most potent compounds exceeded the activity of combretastatin
Takashi Kozaka et al.
Bioorganic & medicinal chemistry letters, 20(14), 4091-4094 (2010-06-15)
As a part of our continuing study of colchicinoids as therapeutically useful antitumor drugs, thiocolchicine derivatives, including their phosphate and other water soluble salts, were synthesized and evaluated for inhibition of tubulin polymerization and for in vitro cytotoxicity. Three compounds
Patrizia Diana et al.
Journal of medicinal chemistry, 51(8), 2387-2399 (2008-03-28)
Isoindoloquinoxalines 4 and 5 were obtained by refluxing 2-(2'-aminoaryl)-1-cyanoisoindoles 3a- e in acetic or formic acid. All derivatives were screened by the National Cancer Institute (Bethesda, MD) for the in vitro one dose primary anticancer assay against a 3-cell line
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