title: Synthesis and bioactivity of a Goralatide analog with antileukemic activity.
abstract: Natural tetrapeptide Goralatide (AcSDKP) is a selective inhibitor of primitive haematopoietic cell proliferation. It is not stable in vivo and decomposes within 4.5min when applied to live cells. In this work we developed an analog of Goralatide that exhibits cytotoxicity towards human myeloid HL-60, HEL, Nalm-6 leukemia cells, endothelial HUVEC, glioblastoma U251 and transformed kidney 293T cells. The Goralatide analog showed significant stability in organic solution with no tendency to degrade oxidatively.
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States.
authors.forename: Zhiliang
authors.initials: Z
authors.lastname: Li
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States; Department of Chemistry and Physics, Georgia Regents University, 1120 15th Street SCI W3005, Augusta, GA 30912, United States.
authors.forename: Iryna O
authors.initials: IO
authors.lastname: Lebedyeva
authors.affiliation: Department of Surgical Oncology, Roswell Park Cancer Institute, Buffalo, NY 14263, United States.
authors.forename: Vita M
authors.initials: VM
authors.lastname: Golubovskaya
authors.affiliation: Department of Surgical Oncology, Roswell Park Cancer Institute, Buffalo, NY 14263, United States.
authors.forename: William G
authors.initials: WG
authors.lastname: Cance
authors.affiliation: Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Alamry
authors.affiliation: Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
authors.forename: Hassan M
authors.initials: HM
authors.lastname: Faidallah
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States. Electronic address: charlesdennishall@gmail.com.
authors.forename: C
authors.initials: C
authors.lastname: Dennis Hall
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States.
authors.forename: Alan R
authors.initials: AR
authors.lastname: Katritzky
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D057809:HEK293 Cells; D018922:HL-60 Cells; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D009842:Oligopeptides; C058504:goralatide
keywords: Anticancer; Antileukemic; Goralatide; Peptide; Peptidomimetic