Antiproliferative activity in HL60 cells by tetrasubstituted pyrroles: a structure-activity relationship study.
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.
Padrón
José M
JM
Unidad de Investigación, Hospital Universitario NS de Candelaria, Ctra. del Rosario s/n, 38010 Santa Cruz de Tenerife, Spain. jmpadron@ull.es
Tejedor
David
D
Santos-Expósito
Alicia
A
García-Tellado
Fernando
F
Martín
Víctor S
VS
Villar
Jesús
J
D002455:Cell Division / Q000187:drug effects*; D018922:HL-60 Cells; D006801:Humans; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D011758:Pyrroles