Abstract:
:To study the effect of substituents on the antitumor activities of analogs of 1-phenyl-3-benzyl-3-methyltriazenes, a series of compounds was designed and synthesized in which the substituent on the 1-phenyl was an electron-withdrawing group and the substituent on the 3-benzyl had a broad range of physicochemical properties. Of the 13 analogs prepared and tested against Sarcoma-180 in the mouse, five showed significant activity. The results were submitted to discriminant analysis to determine structure-activity relationships.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Dunn WJ 3rd,Greenberg MJdoi
10.1002/jps.2600661017subject
Has Abstractpub_date
1977-10-01 00:00:00pages
1416-9issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)39590-3journal_volume
66pub_type
杂志文章abstract::Most of the global healthcare issues facing us--from expanding access to care, to providing medical and dental care in the aftermath of disasters--are far too complex for any single sector to successfully solve. Industry, the healthcare profession, government, academia and non-governmental organizations (NGOs) are all...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21557
更新日期:2008-12-01 00:00:00
abstract::Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1016/j.xphs.2018.03.009
更新日期:2018-07-01 00:00:00
abstract::The presence of subvisible particles in formulations of therapeutic proteins is a risk factor for adverse immune responses. Although the immunogenic potential of particulate contaminants likely depends on particle structural characteristics (e.g., composition, size, and shape), exact structure-immunogenicity relations...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.01.015
更新日期:2018-05-01 00:00:00
abstract::Twenty-two neutral, lipid-soluble 99mTc complexes have been synthesized from diamine dithiol (DADT) ligands which vary in alkyl substitution pattern on nitrogen and carbon. The logarithm of the partition coefficients (log PC), as well as the capacity factor k', of the purified complexes increased linearly with molecul...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600830609
更新日期:1994-06-01 00:00:00
abstract::The relationship between chemical structure and antifungal activity of quaternary imidazolium compounds is analyzed. The compounds are described by a set of condition attributes concerning structure and by a decision attribute concerning activity. The description builds up an information system. The smallest set of co...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840225
更新日期:1995-02-01 00:00:00
abstract::Near infrared (NIR) spectroscopy was used for quantitatively monitoring polymorph conversion of an active pharmaceutical ingredient (API) in wet granulation. The API under pharmaceutical development has two different polymorphs. Polymorph A is the stable form for drug development and polymorph B is the undesired form ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20501
更新日期:2005-12-01 00:00:00
abstract::There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.10.065
更新日期:2019-01-01 00:00:00
abstract::This edition of the Journal of Pharmaceutical Sciences is dedicated to the wonderful career of Per Artursson from the Uppsala University. My Commentary focusses on Per's major contributions to the Caco-2 cell literature over the past 30 years. Two especially influential papers have been cited more than 1000 times out ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.08.016
更新日期:2021-01-01 00:00:00
abstract::The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700930
更新日期:1981-09-01 00:00:00
abstract::In this paper, we demonstrate that by employing a combination of sedimentation field-flow fractionation (sedFFF) and other characterization techniques, such as photon correlation spectroscopy (PCS) and freeze-fracture electron microscopy (EM), it is possible to show that commercial fat emulsions of similar overall che...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600831114
更新日期:1994-11-01 00:00:00
abstract::Angiogenesis--process of new blood-vessel growth from existing vasculature--is an integral part of both normal developmental processes and numerous pathologies such as cancer, ischemic diseases and chronic inflammation. Angiogenesis plays a crucial role facilitating tumour growth and the metastatic process, and it is ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.21286
更新日期:2008-10-01 00:00:00
abstract::Baclofen immediate release mode of administration exhibit sharp plasma peaking that results in the emergence of side effects like hypotension. This research employs preformulation studies to design an optimum dosage form for baclofen to enhance therapeutic outcomes. These studies include partition coefficient and ex-v...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.10.025
更新日期:2020-10-15 00:00:00
abstract::Daunorubicin (DAUN) and doxorubicin (DOX) are used to treat a variety of cancers. The use of DAUN and DOX is hampered by the development of cardiotoxicity. Clinical evidence suggests that patients with leukemia and Down syndrome are at increased risk for anthracycline-related cardiotoxicity. Carbonyl reductases and al...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.03.013
更新日期:2016-06-01 00:00:00
abstract::(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and l...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23062
更新日期:2012-05-01 00:00:00
abstract::Blood levels of intact chloroprocaine were determined using a GLC procedure capable of detecting as little as 10 ng of chloroprocaine/ml of blood. It was necessary to detective plasma cholinesterases in collected samples by adding echothiophate iodide to blood sampling tubes. An extraction procedure, followed by a TLC...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600680123
更新日期:1979-01-01 00:00:00
abstract::A spectrodensitometric assay was developed for propranolol based on measurement of the absorbance of the drug on silica gel plates irradiated at 822 nm. Quantities as low as 0.10 microgram can be detected, and a linear relationship was obtained between 0.010 and 0.400 microgram. The percent recovery from plasma spiked...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670931
更新日期:1978-09-01 00:00:00
abstract::The disposition of the beta-blocking drug talinolol is controlled by P-glycoprotein in man. Because talinolol is marketed as a racemate, we reevaluated the serum-concentration time profiles of talinolol of a previously published study with single intravenous (30 mg) and repeated oral talinolol (100 mg for 14 days) bef...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10054
更新日期:2002-02-01 00:00:00
abstract::Transcutaneous immunization is the administration of a vaccine on the skin to generate efficient systemic and mucosal immune responses against an antigen. In the present study, reconstituted hepatitis B surface antigen vesicles (HBsAg-REVs) integrated with monophosphoryl lipid A were prepared by the delipidation-recon...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2019.07.007
更新日期:2019-11-01 00:00:00
abstract::The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of the tongue, to investigate the mechanisms of glucose uptake. The uptake of D-glucose was much larger in cells of the dorsum of the tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章
doi:10.1021/js980298f
更新日期:1999-08-01 00:00:00
abstract::Plasma and various organ concentrations of canrenone, canrenoate, and total 3H-activity were measured following single doses of 20 mg of 3H-canrenoate/kg iv to rabbits. Organs studied included heart, lungs, brain, kidneys, liver, adrenal glands, and spleen. Canrenoate was shown to be in rapid equilibrium with canrenon...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660237
更新日期:1977-02-01 00:00:00
abstract::A sensitive, simple, and rapid method for the quantitation of ibuprofen in plasma, using 1-(p-fluorobenzoyl)-5-methoxy-2-methylindole acetic acid as the internal standard, was developed. The method is based on reversed-phase high-pressure liquid chromatography with a mobile phase containing acetonitrile--0.1 M acetic ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700829
更新日期:1981-08-01 00:00:00
abstract::This study describes a fast spectrophotometic titration method for apparent ionization constant (pKa) determination. In this method, a Universal pH indicator is utilized instead of the conventional pH electrode. An autoburette is set to add HCl at a constant rate to a vigorously stirred 1 cm UV cuvette which contains ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20959
更新日期:2007-10-01 00:00:00
abstract::Griseofulvin/cyclodextrin interactions were investigated in aqueous environment and in solid state. Two cyclodextrin derivatives (beta-cyclodextrin and 2-hydroxypropyl beta-cyclodextrin) were used to prepare different physical mixtures and kneaded systems, and the drug/cyclodextrin ratios were 1:1 and 1:2 mol/mol. Sca...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js970233x
更新日期:1998-07-01 00:00:00
abstract::Cytochrome P450 1B1 (CYP1B1) has been reported to have a major role in metabolizing arachidonic acid (AA) into cardiotoxic metabolites, mid-chain hydroxyeicosatetraenoic acids (HETEs). Recently, we have shown that fluconazole decreases the level of mid-chain HETEs in human liver microsomes. Therefore, the objectives o...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.03.016
更新日期:2020-07-01 00:00:00
abstract::The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23145
更新日期:2012-07-01 00:00:00
abstract::A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600731245
更新日期:1984-12-01 00:00:00
abstract::A rapid and accurate method for the quantitative determination of the extent and ratio of amino and carboxyl group trimethylsilylation of 6-aminopenicillanic acid, 7-amino-3-methyl-delta3-cephem-4-carboxylic acid, and 7-amino-3-acetoxymethyl-delta3-cephem-4-carboxylic acid is presented. The method utilizes NMR spectro...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600661230
更新日期:1977-12-01 00:00:00
abstract::A tetrazole ring is often used in drug discovery as a replacement for the carboxylic acid group. Previous work indicates that compounds containing a tetrazole moiety show asymmetric permeability in Caco-2 cells characteristic of an efflux transporter substrate. The aim of this study is to determine which transporters ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20526
更新日期:2006-04-01 00:00:00
abstract::Sugars and polyols have been used routinely with lyophilized proteins and peptides as bulking agents, cryoprotectants, and lyoprotectants. However, reducing sugars may present a problem as excipients since they are potentially reactive with proteins. In this stability study of recombinant human relaxin (Rix) with vari...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js950456s
更新日期:1996-08-01 00:00:00
abstract::In the present study, the interaction between phenobarbital and activated carbons which is driven by hydrophobic bonding was evaluated. The Two-Mechanism Langmuir-Like Equation was proposed to describe the isotherms for phenobarbital adsorbing to activated carbons. The parameters in the Two-Mechanism Langmuir-Like Equ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.06.018
更新日期:2019-01-01 00:00:00