RRC ID 58648
著者 Alexander BE, Sun S, Palframan MJ, Kociok-Köhn G, Dibwe DF, Watanabe S, Caggiano L, Awale S, Lewis SE.
タイトル Sidechain Diversification of Grandifloracin Allows Identification of Analogues with Enhanced Anti-Austerity Activity against Human PANC-1 Pancreatic Cancer Cells.
ジャーナル ChemMedChem
Abstract The natural product (+)-grandifloracin is a potent "anti-austerity" agent, able to suppress the ability of various pancreatic cancer cell lines to tolerate conditions of nutrient deprivation. Such anti-austerity agents represent a promising approach to cancer chemotherapy. Here we report the synthesis and biological evaluation of racemic analogues of grandifloracin bearing diverse sidechains, of which two show enhanced potency in comparison with the natural product. Additionally, several unexpected by-products containing modifications of the grandifloracin core were isolated, identified and similarly evaluated for biological activity.
巻・号 15(1)
ページ 125-135
公開日 2020-1-7
DOI 10.1002/cmdc.201900549
PMID 31821731
PMC PMC7003952
MeSH Antineoplastic Agents, Phytogenic / chemical synthesis Antineoplastic Agents, Phytogenic / chemistry* Antineoplastic Agents, Phytogenic / pharmacology Biological Products / chemical synthesis Biological Products / chemistry Biological Products / pharmacology Bridged-Ring Compounds / chemical synthesis Bridged-Ring Compounds / chemistry* Bridged-Ring Compounds / pharmacology Cell Line, Tumor Cell Survival / drug effects Crystallography, X-Ray Humans Molecular Conformation Pancreatic Neoplasms / metabolism Pancreatic Neoplasms / pathology Stereoisomerism
IF 3.124
引用数 0
リソース情報
ヒト・動物細胞 PANC-1(RCB2095)