Journal ArticleDOI
Synthesis and biological evaluation of cyclopenta[c]thiophene related compounds as new antitumor agents.
Patrick Dallemagne,Lan Pham Khanh,Abdellah Alsaïdi,Renault Olivier,Isabelle Varlet,Valérie Collot,Ronan Bureau,Sylvain Rault +7 more
TLDR
A series of 22 cyclopenta[c]thiophene related compounds were obtained by the pharmacomodulation of 6-amino-5,6-dihydro-4H-cyclopenta-4-ones 1a-g as discussed by the authors.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2002-07-01. It has received 28 citations till now.read more
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Thiophene-based derivatives as anticancer agents: An overview on decade's work.
TL;DR: The present review has presented the information available on thiophene-based molecules as anticancer agents with special focus on synthetic methodologies, biological profile and structure activity relationship (SAR) studies.
Journal ArticleDOI
Synthesis and biological evaluation of five-membered heterocycles fused to cyclopenta[c]thiophene as new antitumor agents.
Patrick Dallemagne,Lan Pham Khanh,Abdellah Alsaïdi,Isabelle Varlet,Valérie Collot,Magalie Paillet,Ronan Bureau,Sylvain Rault +7 more
TL;DR: The oxazolidinone derivatives 2a-c displayed further in vivo antitumor activity in the hollow fiber assay and standard xenograft testing developed at the NCI.
Journal ArticleDOI
Synthesis, biological evaluation and 3D-QSAR study of novel 4,5-dihydro-1H-pyrazole thiazole derivatives as BRAFV600E inhibitors
Meng-Yue Zhao,Yong Yin,Xiao-Wei Yu,Chetan B. Sangani,Shu-Fu Wang,Aimin Lu,Lifang Yang,Peng-Cheng Lv,Mingguo Jiang,Hai-Liang Zhu +9 more
TL;DR: A series of novel 4,5-dihydro-1H-pyrazole derivatives containing thiazole moiety as potential V600E mutant BRAF kinase (BRAF(V600E))) inhibitors designed and synthesized revealed that compound 10d was bearing the best bioactivity and could induce remarkable apoptosis of MCF-7 and WM266.4 cells in a dose dependent manner.
Journal ArticleDOI
THERMOCHEMICAL STUDY OF 2- AND 3-ALKYL SUBSTITUTED THIOPHENES Energetic-structural correlations
TL;DR: In this paper, the standard molar enthalpies of combustion, in oxygen, to yield CO2(g) and H2SO4·115H2O(aq), measured by rotating-bomb combustion calorimetry, were derived.
References
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Journal ArticleDOI
Some Practical Considerations and Applications of the National Cancer Institute In Vitro Anticancer Drug Discovery Screen
Michael R. Boyd,Kenneth D. Paull +1 more
TL;DR: Practical considerations and selected specific examples are selected, particularly illustrating research applications of the NCI screen that may be more broadly applicable to the search for new anticancer drug development leads with novel profiles of antitumor activity and/or mechanisms of action.
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Display and Analysis of Patterns of Differential Activity of Drugs Against Human Tumor Cell Lines: Development of Mean Graph and COMPARE Algorithm
Kenneth D. Paull,Robert H. Shoemaker,Louis Hodes,Anne Monks,Dominic A. Scudiero,Larry Rubinstein,Jacqueline Plowman,Michael R. Boyd +7 more
TL;DR: This study developed a key methodological tool, the mean graph, which allowed the transformation of the numerical cell line response data into graphic patterns that were particularly expressive of differential cell growth inhibition.
Journal ArticleDOI
In vivo cultivation of tumor cells in hollow fibers.
Melinda G. Hollingshead,Michael C. Alley,Richard F. Camalier,B. J. Abbott,Joseph G. Mayo,Louis Malspeis,Michael R. Grever +6 more
TL;DR: Results of experimentation to date demonstrate that a hollow fiber encapsulation/implantation methodology provides quantitative indices of drug efficacy with minimum expenditures of time and materials.
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Researches on Pyrimidines. CXLIX. The Synthesis of Aryl Substituted Dihydrouracils and their Conversion to Uracil Derivatives1
Treat B. Johnson,John E. Livak +1 more