Antiproliferative activity in HL60 cells by tetrasubstituted pyrroles: A structure-activity relationship study

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 10, 2005, Pages 2487-2490

  Padrón, José M ^a,d   Tejedor, David ^b,d   Santos Expósito, Alicia ^b   García Tellado, Fernando ^b   Martín, Víctor S ^c,d   Villar, Jesús ^a  

^a HOSPITAL UNIVERSITARIO NUESTRA SEÑORA DE CANDELARIA   (Spain)

^b INSTITUTO DE PRODUCTOS NATURALES Y AGROBIOLOGÍA   (Spain)

^c UNIVERSIDAD DE LA LAGUNA   (Spain)

^d Madrid Spain   (Spain)

Author keywords

Antitumor drugs; Leukemia; Privileged structure; Pyrroles

Indexed keywords

AMINE; PYRROLE DERIVATIVE; SILICA GEL;

ARTICLE; CELL PROLIFERATION; CONJUGATION; CONTROLLED STUDY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; IRRADIATION; LEUKEMIA CELL; PROMYELOCYTIC LEUKEMIA; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

EID: 18144406522     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.03.069     Document Type: Article

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18. Pure compounds were initially dissolved in DMSO at 400 times the desired final maximum test concentration, that is, 100 μM. Control cells were exposed to an equivalent concentration of DMSO. Each agent was tested in duplicates at five different 10-fold dilutions. Drug incubation times were 48 h, after which cells were precipitated with 50 μL ice-cold 80% (w/v) trichloroacetic acid and fixed for 60 min at 4°C. Then the SRB assay was performed. The optical density (OD) of each well was measured at 490 nm using Bio-Tek's Elx800 NB 96-well plate reader. The percentage growth was calculated at each of the drug concentration levels based on the difference in OD at the start and end of drug exposure. Values were corrected for background OD from wells only containing medium