Recent progress with microtubule stabilizers: new compounds, binding modes and cellular activities
TLDR
Recent progress in the chemistry and biology of these diverse microtubule stabilizers focusing on the wide range of organisms that produce these compounds, their mechanisms of inhibiting microtubules-dependent processes, mechanisms of drug resistance, and their interactions with tubulin including their distinct binding sites and modes are covered.About:
This article is published in Natural Product Reports.The article was published on 2014-02-11 and is currently open access. It has received 113 citations till now.read more
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Pyridine Moiety: Recent Advances in Cancer Treatment
TL;DR: This review throws light on recent biological expansions of pyridine along with their structure activity relationships/molecular docking to deliver association between various synthesized newer derivatives and receptor sites.
Journal ArticleDOI
Synthesis and Biological Evaluation of New Antitubulin Agents Containing 2-(3′,4′,5′-trimethoxyanilino)-3,6-disubstituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine Scaffold
Romeo Romagnoli,Filippo Prencipe,Paola Oliva,Barbara Cacciari,Jan Balzarini,Sandra Liekens,Ernest Hamel,Andrea Brancale,Salvatore Ferla,Stefano Manfredini,Matteo Zurlo,Alessia Finotti,Roberto Gambari +12 more
TL;DR: The cell apoptosis study found that compounds 3a and 3b were very effective in the induction of apoptosis in a dose-dependent manner and did not induce cell death in normal human peripheral blood mononuclear cells, suggesting that they may be selective against cancer cells.
Journal ArticleDOI
Synthesis and Biological Investigation of Bile Acid-Paclitaxel Hybrids
Elisabetta Melloni,Elena Marchesi,Lorenzo Preti,Fabio Casciano,Erika Rimondi,Arianna Romani,Paola Secchiero,Maria Luisa Navacchia,Daniela Perrone +8 more
TL;DR: Flow cytometry clearly showed that both CDCA and UDCA conjugation to PTX improved its incoming into HCT116 cells, allowing the derivatives to enter the cells up to 99.9%, respect to 35% in the case of PTX.
Journal ArticleDOI
3-Vinylazetidin-2-Ones: Synthesis, antiproliferative and tubulin destabilizing activity in MCF-7 and MDA-MB-231 Breast Cancer Cells
Shu Wang,Azizah M. Malebari,Azizah M. Malebari,Thomas F Greene,Niamh M. O’Boyle,Darren Fayne,Seema M. Nathwani,Brendan Twamley,Thomas McCabe,Niall O. Keely,Daniela M. Zisterer,Mary J. Meegan +11 more
TL;DR: A series of 3-vinyl-β-lactams (2-azetidinones) were designed, synthesized and evaluated as potential tubulin polymerization inhibitors, and for their antiproliferative effects in breast cancer cells.
Journal ArticleDOI
Indazole-based microtubule-targeting agents as potential candidates for anticancer drugs discovery.
Dilipkumar Pal,In-Ho Song,Shrikant Dashrath Warkad,Keum-Soo Song,Gyu Seong Yeom,Supriyo Saha,Pramod B. Shinde,Satish Balasaheb Nimse +7 more
TL;DR: In this article , the authors present the advances in research on compounds containing indazole scaffolds as microtubule targeting agents based on the articles published in the last two decades, and find that compounds 6 and 7 showed the lowest IC50 values of 0.6 ∼ 0.9 nM in the cell line studies.
References
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Microtubules as a target for anticancer drugs.
Mary Ann Jordan,Leslie Wilson +1 more
TL;DR: Highly dynamic mitotic-spindle microtubules are among the most successful targets for anticancer therapy, and it is now known that at lower concentrations, microtubule-targeted drugs can suppress micro Tubule dynamics without changingmicrotubule mass; this action leads to mitotic block and apoptosis.
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Microtubule-binding agents: a dynamic field of cancer therapeutics
Charles Dumontet,Mary Ann Jordan +1 more
TL;DR: The screening of a range of botanical species and marine organisms has yielded promising new antitubulin agents with novel properties, and the three main objectives are enhanced tumour specificity, reduced neurotoxicity and insensitivity to chemoresistance mechanisms.
Journal Article
Epothilones, a New Class of Microtubule-stabilizing Agents with a Taxol-like Mechanism of Action
Daniel M. Bollag,Patricia A. McQueney,Jian Zhu,Otto D. Hensens,Lawrence R. Koupal,Jerrold M. Liesch,Michael A. Goetz,Elias Lazarides,Catherine M. Woods +8 more
TL;DR: Epothilones represent a novel structural class of compounds, the first to be described since the original discovery ofTaxol, which not only mimic the biological effects of taxol but also appear to bind to the same microtubule-binding site as taxol.
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