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 μM, and only six products showed TGI values within the evaluation range. A structure–activity relationship is also discussed.

The synthesis of tetrasubstituted pyrrole derivatives 2 and their in vitro antiproliferative activity against HL60 cells is reported.Figure optionsDownload as PowerPoint slide