Huang, David S.; Wong, Henry L.; Georg, Gunda I. published the artcile< Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin>, Related Products of 171877-39-7, the main research area is pironetin analog preparation anticancer structure activity ovarian cancer; Cytotoxicity; Pironetin; Structure-activity; Synthesis; Tubulin.
Pironetin is an α-tubulin-binding natural product with potent antiproliferative activity against several cancer cell lines that inhibits cell division by forming a covalent adduct with α-tubulin via a Michael addition into the natural product’s α,β-unsaturated lactone. We designed and prepared analogs carrying electron-withdrawing groups at the α-position (C2) of the α,β-unsaturated lactone with the goal to generate potent and selective binding analogs. We prepared derivatives I (R = F, Me, Cl, Br, Ph) containing halogens, a Ph, and a Me group at the C2 position to evaluate the structure-activity relationship at this position. Testing of the analogs in ovarian cancer cell lines demonstrated 100-1000-fold decreased antiproliferative activity.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Related Products of 171877-39-7.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica