title: Antiproliferative activity in HL60 cells by tetrasubstituted pyrroles: a structure-activity relationship study.
abstract: A number of tetrasubstituted pyrrole derivatives have been synthesized and evaluated for their in vitro antiproliferative activities using the human promyelocytic leukemia cell line HL60. Tetrasubstituted pyrroles are obtained by irradiation of a silica gel absorbed mixture of a conjugated alkynoate and a primary amine. Active compounds exhibited GI50 values in the range 4-45 microM, and only six products showed TGI values within the evaluation range. A structure-activity relationship is also discussed.
authors.affiliation: Unidad de Investigación, Hospital Universitario NS de Candelaria, Ctra. del Rosario s/n, 38010 Santa Cruz de Tenerife, Spain. jmpadron@ull.es
authors.forename: José M
authors.initials: JM
authors.lastname: Padrón
authors.forename: David
authors.initials: D
authors.lastname: Tejedor
authors.forename: Alicia
authors.initials: A
authors.lastname: Santos-Expósito
authors.forename: Fernando
authors.initials: F
authors.lastname: García-Tellado
authors.forename: Víctor S
authors.initials: VS
authors.lastname: Martín
authors.forename: Jesús
authors.initials: J
authors.lastname: Villar
mesh_terms: D002455:Cell Division / Q000187:drug effects*; D018922:HL-60 Cells; D006801:Humans; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011758:Pyrroles