Tubulin colchicine site binding agent LL01 displays potent antitumor efficiency both in vitro and in vivo with suitable drug-like properties
Sign Up to like & getrecommendations! Published in 2019 at "Investigational New Drugs"
DOI: 10.1007/s10637-019-00753-z
Abstract: Through rational drug design, we previously identified an indenoprazole derivative, 2-(6-ethoxy-3-(3-ethoxyphenylamino)-1-methyl-1,4-dihydroindeno[1,2- c ]pyrazol-7-yloxy)acetamide (LL01), as a potent tubulin polymerization inhibitor targeting the tubulin colchicine binding site. In this study, we further demonstrated that LL01 was… read more here.
Keywords: site binding; drug; ll01; tubulin colchicine ... See more keywords
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
1-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.04.040
Abstract: The colchicine site inhibitors (CSIs) showed promising prospects as antitumor agents due to their vascular disrupting activities besides antimitotic activities. 1-Phenyl-dihydrobenzoindazole was found as a novel scaffold of CSI without the cis-trans isomerization problem. The… read more here.
Keywords: phenyl dihydrobenzoindazoles; site inhibitors; antitumor; colchicine site ... See more keywords
β-III Tubulin Levels Determine the Neurotoxicity Induced by Colchicine-Site Binding Agent Indibulin.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.2c00324
Abstract: Indibulin, a microtubule-depolymerizing agent, produces minimal neurotoxicity in animals. It is also less cytotoxic toward differentiated neuronal cells than undifferentiated cells. We found that the levels of β-III tubulin, acetylated tubulin, and polyglutamylated tubulin were… read more here.
Keywords: tubulin; iii tubulin; indibulin; colchicine site ... See more keywords
Phytochemical and Pharmacophoric Fragment Based Anticancer Drug Development.
Sign Up to like & getrecommendations! Published in 2020 at "Current computer-aided drug design"
DOI: 10.2174/1573409916666200212122445
Abstract: BACKGROUND Cancer is the leading cause of death in the current decade. With the advancement in scientific technologies various treatments had been introduced but they suffer from numerous side effects. The root cause of cancer… read more here.
Keywords: site microtubules; drug; colchicine site; anticancer ... See more keywords