RT Journal Article
T1 In Vitro Primary Screening of a Synthetic Series of Chromenoazoldiones against  Trypanosoma cruzi
A1 Fonseca Berzal, Cristina Rosa
A1 Morales, Paula
A1 Escario García-Trevijano, José Antonio
A1 Gómez Barrio, Alicia
A1 Jagerovic, Nadine
AB Similarities between parasites  and  cancer have prompted parasitologists to take  advantage  of several approaches enabled by  cancer  research  to  identify  antiparasitic agents  [1]. Quinones generate reactive oxygen species (ROS),  which not  only results in  their  antitumor properties, but also in  a mechanism  for designing  antichagasic  drugs. Here,  a synthetic series of  seven  chromenoazoldiones previously  defined  as  potential  antitumorals  [2,3],  has been  assayed in vitro  against  Trypanosoma  cruzi (CL-B5  lacZ  strain) in  a  primary screening that  evaluates  activity over epimastigotes and toxicity on L929  cells  [4,5].  Compounds  PM199,  PM203  and  PM401  achieved  higher  IC50  values than  that  of the reference drug  benznidazole (BZ):  IC50  =  14.45  ± 1.90, 14.84  ± 4.49, 16.01  ± 9.06  and 36.47  ± 4.43  µM (PM199, PM203, PM401 and BZ, respectively). However, their  higher cytotoxicity  led to  a  lower selectivity  (SI)  on  epimastigotes:  SIPM199  = 5.83,  SIPM203  = 7.03,  SIPM401  = 5.27  and  SIBZ  > 7.02.  Only  two compounds  showed no  cytotoxicity (LC50  > 256  µM)  and thus, no derivative  was further  assayed against  intracellular  amastigotes. These  chromenoazoldiones did  not show relevant activity on  T. cruzi. Their cytotoxicity, probably  connected to ROS production in mammalian cells, encourages further optimization to  apply them  as  trypanocidal  templates.
PB MDPI
SN 2504-3900
YR 2017
FD 2017-10-17
LK https://hdl.handle.net/20.500.14352/19233
UL https://hdl.handle.net/20.500.14352/19233
LA eng
NO Fonseca Berzal, C., Morales, P., Escario Garcia-Trevijano, J. A. et al. «In Vitro Primary Screening of a Synthetic Series of Chromenoazoldiones against Trypanosoma Cruzi». Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, MDPI, 2017, p. 650. DOI.org (Crossref), https://doi.org/10.3390/proceedings1060650.
NO Ministerio de Economía, Comercio y Empresa (España)
NO CEI Campus Moncloa (UCM-UPM & CSIC)
NO Universidad Complutense de Madrid
DS Docta Complutense
RD 11 may 2025