Tubulin inhibitors: Discovery of a new scaffold targeting extra-binding residues within the colchicine site through anchoring substituents properly adapted to their pocket by a semi-flexible linker.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103767
Abstract: Bis-hydrazides 13a-h were designed and synthesized as potential tubulin inhibitors selectively targeting the colchicine site between α- and β-tubulin subunits. The newly designed ring-B substituents were assisted at their ends by 'anchor groups' which are… read more here.
Keywords: tubulin inhibitors; tubulin; extra binding; colchicine site ... See more keywords
Emerging treatment using tubulin inhibitors in advanced non-small cell lung cancer
Sign Up to like & getrecommendations! Published in 2017 at "Expert Opinion on Pharmacotherapy"
DOI: 10.1080/14656566.2017.1316374
Abstract: ABSTRACT Introduction: Tubulin inhibitors including taxanes and vinca alkaloids are important components of chemotherapy regimens used in advanced non-small cell lung cancer (NSCLC). Despite a treatment paradigm shift due to molecularly-targeted therapies and immunotherapy, a… read more here.
Keywords: treatment; tubulin inhibitors; lung cancer;
In Silico Exploration of Novel Tubulin Inhibitors: A Combination of Docking and Molecular Dynamics Simulations, Pharmacophore Modeling, and Virtual Screening
Sign Up to like & getrecommendations! Published in 2022 at "Computational and Mathematical Methods in Medicine"
DOI: 10.1155/2022/4004068
Abstract: Microtubules play a critical role in mitosis and cell division and are regarded as an excellent target for anticancer therapy. Although microtubule-targeting agents have been widely used in the clinical treatment of different human cancers,… read more here.
Keywords: tubulin inhibitors; molecular dynamics; pharmacophore model; docking molecular ... See more keywords
Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12121843
Abstract: Cancer accounts for numerous deaths each year, and it is one of the most common causes of death worldwide, despite many breakthroughs in the discovery of novel anticancer candidates. Each new year the FDA approves… read more here.
Keywords: binding site; tubulin inhibitors; colchicine binding; cancer ... See more keywords
Structure-Based Pharmacophore Design and Virtual Screening for Novel Tubulin Inhibitors with Potential Anticancer Activity
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DOI: 10.3390/molecules24173181
Abstract: Tubulin inhibitors have been considered as potential drugs for cancer therapy. However, their drug resistance and serious side-effects are the main reasons for clinical treatment failure. Therefore, there is still an urgent need to develop… read more here.
Keywords: virtual screening; based pharmacophore; tubulin inhibitors; screening ... See more keywords
Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27051587
Abstract: Tubulin inhibitors can interfere with normal cell mitosis and inhibit cell proliferation through interfering with the normal structure and function of microtubules, forming spindle filaments. Indole, as a privileged pharmacological skeleton, has been widely used… read more here.
Keywords: tubulin inhibitors; based tubulin; modes sars; tubulin ... See more keywords