Journal ArticleDOI
Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-β-carbolines
Marie Laronze,Michel Boisbrun,Stéphane Léonce,Bruno Pfeiffer,Pierre Renard,Olivier Lozach,Laurent Meijer,Amélie Lansiaux,Christian Bailly,Janos Sapi,J.-Y. Laronze +10 more
TLDR
In this paper, pyrrolidino-fused (aza) carbazoles were prepared and screened towards a few cancer-related targets, including 28a and 28a derivatives.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2005-03-15. It has received 79 citations till now.read more
Citations
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Recent trends in targeted anticancer prodrug and conjugate design.
TL;DR: The present review highlights recent trends in prodrug and conjugate rationale and design for cancer treatment and critically analyzed the various approaches that are currently being explored.
Journal ArticleDOI
Synthesis and cytotoxic activities of β-carboline amino acid ester conjugates
Ming Zhao,Lanrong Bi,Lanrong Bi,Wei Wang,Wei Wang,Chao Wang,Chao Wang,Michèle Baudy-Floc’h,Michèle Baudy-Floc’h,Jingfang Ju,Jingfang Ju,Shiqi Peng,Shiqi Peng +12 more
TL;DR: New insights into structure-activity relationships in the beta-carboline amino acid ester conjugates are provided and the Lys/Arg conjugating compounds are identified as promising lead compounds for further in vivo biological and molecular evaluation.
Journal ArticleDOI
Novel N-(3-carboxyl-9-benzyl-β-carboline-1-yl)ethylamino acids: Synthesis, anti-tumor evaluation, intercalating determination, 3D QSAR analysis and docking investigation
TL;DR: Sixteen novel N-(3-carboxyl-9-benzyl-beta-carboline-1-yl)ethylamino acids (6a-p) were synthesized as intercalating lead compounds and the relationship of the in vivo anti-tumor activity and the structure was quantitatively described.
Journal ArticleDOI
Acid‐Free Synthesis of Carbazoles and Carbazolequinones by Intramolecular Pd‐Catalyzed, Microwave‐Assisted Oxidative Biaryl Coupling Reactions – Efficient Syntheses of Murrayafoline A, 2‐Methoxy‐3‐methylcarbazole, and Glycozolidine
TL;DR: In this paper, a mild and efficient methodology for the synthesis of oxygenated carbazoles from diarylamines under non-acidic conditions was developed, based on a palladium-catalyzed, microwave-assisted double C-H bond activation process.
Journal ArticleDOI
Microwave-assisted synthesis of N-substituted cyclic imides and their evaluation for anticancer and anti-inflammatory activities
TL;DR: These compounds were screened for anticancer and anti-inflammatory activities, and compounds 3c, 3e, 5c, 9c, and 9d exhibited anticancer activity against colon (COLO 205) cancer better than 5-fluorouracil and mitomycin-C, and compound 9b exhibited anti- inflammatory activity better than standard drug phenyl butazone.
References
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Protein kinase inhibitors: insights into drug design from structure.
TL;DR: This review focuses on kinase inhibitors that are in the clinic or in clinical trials and for which structural information is available and which have provided insights into targeting the inactive or active form of the kinase, for targeting the global constellation of residues at the ATP site, and into targeting noncatalytic domains.
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Isolation and synthesis of biologically active carbazole alkaloids
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GSK3 inhibitors: development and therapeutic potential
Philip Cohen,Michel Goedert +1 more
TL;DR: The biology of GK3 relevant to its potential as a target for diabetes and neurodegenerative diseases is described, and progress in the development of GSK3 inhibitors is discussed.
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Pharmacological inhibitors of cyclin-dependent kinases
TL;DR: Pharmacological inhibitors of CDKs are currently being evaluated for therapeutic use against cancer, alopecia, neurodegenerative disorders, cardiovascular disorders, viral infections and parasitic protozoa.
Journal ArticleDOI
4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methyl-morpholinium chloride: an efficient condensing agent leading to the formation of amides and esters
TL;DR: In this paper, 4,6-dimethoxy-1, 3,5-triazin-2(1H)-one was obtained by esterification of caiboxylic acids with DMTMM in methanol, ethanol, isopropy1 alcohol, or t-butyl alcohol.