Design, synthesis and spectroscopic characterisation of a focused library based on the polyandrocarpamine natural product scaffold

Autor:	Lidija Jovanovic, Paul Baron, Lekha Suraweera, Juliette E Neve, David Brian Camp, Colleen C. Nelson, Ann Lam, Rohan A. Davis, John Lai
Rok vydání:	2013
Předmět:	chemistry.chemical_compound Scaffold Natural product chemistry Microwave chemistry Drug discovery In silico Chemical biology General Materials Science Aldol condensation General Chemistry Nuclear magnetic resonance spectroscopy Combinatorial chemistry
Zdroj:	Magnetic Resonance in Chemistry. 51:358-363
ISSN:	0749-1581
DOI:	10.1002/mrc.3958
Popis:	A focused library based on the marine natural products polyandrocarpamines A (1) and B (2) has been designed and synthesised using parallel solution-phase chemistry. In silico physicochemical property calculations were performed on synthetic candidates in order to optimise the library for drug discovery and chemical biology. A library of ten 2-aminoimidazolone products (3-12) was prepared by coupling glycocyamidine and a variety of aldehydes using a one-step stereoselective aldol condensation reaction under microwave conditions. All analogues were characterised by NMR, UV, IR and MS. The library was evaluated for cytotoxicity towards the prostate cancer cell lines, LNCaP, PC-3 and 22Rv1.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::33af6fb521f37c8fcf1f6635a9e17d29 https://doi.org/10.1002/mrc.3958 Zobrazit plný text záznamu Plný text ve formátu PDF