title: The synthesis and anticancer activity of selected diketopiperazines.
abstract: Six selected diketopiperazines, cyclo(Gly-Val), cyclo(Gly-D-Val), cyclo(Gly-Leu), cyclo(Gly-Ile), cyclo(Phe-Cys) and cyclo(Tyr-Cys), were synthesized via various synthetic routes. Their potential to inhibit cancer cell growth in HT-29, HeLa and MCF-7 cells was determined. Cyclo(Tyr-Cys) caused the greatest inhibition in cervical carcinoma cells with near equivalent activity against HT-29 and MCF-7 cells. The other cyclic dipeptides tested were effective in the inhibition of colon, cervical and breast carcinoma cells, respectively, but the percentage inhibition was lower than for cyclo(Tyr-Cys).
authors.affiliation: Department of Pharmacy, Nelson Mandela Metropolitan University, Port Elizabeth 6031, South Africa.
authors.forename: E
authors.initials: E
authors.lastname: van der Merwe
authors.forename: D
authors.initials: D
authors.lastname: Huang
authors.forename: D
authors.initials: D
authors.lastname: Peterson
authors.forename: G
authors.initials: G
authors.lastname: Kilian
authors.forename: P J
authors.initials: PJ
authors.lastname: Milne
authors.forename: M
authors.initials: M
authors.lastname: Van de Venter
authors.forename: C
authors.initials: C
authors.lastname: Frost
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002277:Carcinoma / Q000188:drug therapy*; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D054659:Diketopiperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005260:Female; D019073:HT29 Cells; D006367:HeLa Cells; D006801:Humans; D013058:Mass Spectrometry; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D054659:Diketopiperazines; D010456:Peptides, Cyclic