A novel series of thiazole-naphthalene derivatives as tubulin polymerisation inhibitors were designed, synthesised, and evaluated for the anti-proliferative activities. The majority tested compounds exhibited moderate to potent antiproliferative activity on MCF-7 A549 cancer cell lines. Among them, compound 5b was found be most active with IC50 values 0.48 ± 0.03 0.97 0.13 μM. Moreover, mechani...

Combretastatin A-4 (CA-4) is one of the most potent tubulin polymerization inhibitors. In this paper, the identification of some new CA-4 analogues as potential tubulin polymerization inhibitors is performed by combination of molecular modeling techniques including 3D-QSAR, molecular docking and molecular dynamics (MD) simulation. The built 3D-QSAR models show significant statistical quality an...

Dolastatin 10, a potent antimitotic peptide from a marine animal, strongly inhibits microtubule assembly, tubulin-dependent GTP hydrolysis, and the binding of vinca alkaloids to tubulin. In studies of the binding of [3H]vincristine to the protein, with vinblastine as a control for competitive inhibition (Ki, 6.6 microM), we found that the macrolide antimitotic agents maytansine and rhizoxin wer...

Microtubule inhibitors can be classified into two categories: 1) those which inhibit the polymerization-dependent GTPase activity of phosphocellulose-purified tubulin, but induce a significant polymerization-independent GTPase activity (e.g. colchicine, griseofulvine, daunorubicine); 2) those which inhibit the GTPase activity associated with tubulin polymerization and that induced by inhibitors...

Antibody-drug conjugates (ADCs) are a class of highly potent biopharmaceutical drugs generated by conjugating cytotoxic drugs with specific monoclonal antibodies through appropriate linkers. Specific antibodies used to guide potent warheads to tumor tissues can effectively reduce undesired side effects of the cytotoxic drugs. An in-depth understanding of antibodies, linkers, conjugation strateg...