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Home / Archives for Anticancer Research

Anticancer Research

Thioridazine induces apoptosis of multidrug-resistant mouse lymphoma cells transfected with the human ABCB1 and inhibits the expression of P-glycoprotein.

  • Autores: Amaral L, Molnar J, Spengler G, Viveiros M
  • Ano de Publicação: 2011
  • Journal: Anticancer Research
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Thioridazine+induces+apoptosis+of+multidrug-resistant+mouse+lymphoma+cells+transfected+with+the+human+ABCB1+and+inhibits+the+expression+of+P-glycoprotein

AIM:
Chlorpromazine has activity against a large variety of cancer types. However, this phenothiazine produces a plethora of serious side-effects. We have studied thioridazine (TZ), a phenothiazine neuroleptic that is much milder, for activity against multidrug-resistant (MDR) cancer cells, as well as against the overexpressed ABCB1 transporter (P-glycoprotein) that is the cause for the MDR phenotype of these cancer cells.
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Modulation of multidrug efflux pump activity by new hydantoin derivatives on colon adenocarcinoma cells without inducing apoptosis.

  • Autores: Amaral L, Handzlik J, Kiec-Kononowicz K, Molnar J, Ocsovszki I, Spengler G, Viveiros M
  • Ano de Publicação: 2011
  • Journal: Anticancer Research
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Modulation+of+multidrug+efflux+pump+activity+by+new+hydantoin+derivatives+on+colon+adenocarcinoma+cells+without+inducing+apoptosis

BACKGROUND:
Hydantoin derivatives are very promising candidates to improve the efficacy of anticancer chemotherapy. Previously, we demonstrated that eight hydantoin derivatives inhibited the P-glycoprotein (ABCB1) efflux pump of mouse T-lymphoma cells, as well as acting synergistically with the anticancer drug doxorubicin.
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Rapid, laser-induced conversion of 20-hydroxyecdysone and its diacetonide — experimental set-up of a system for photochemical transformation of bioactive substances.

  • Autores: Alexandru T, Amaral L, Andrei IR, Boni M, Danko B, Hunyadi A, Militaru A, Nastasa V, Pascu ML
  • Ano de Publicação: 2012
  • Journal: Anticancer Research
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/22493361

BACKGROUND:
Photochemical transformation of certain bioactive compounds for the purpose of obtaining derivatives with increased bioactivity is a prospective area of synthetic chemistry. Ecdysteroids, analogs of the insect molting hormone, which can also exert several beneficial effects in mammals including humans, contain an enone moiety in their B ring, and, as such, are good candidates for photochemical transformations.
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In vitro cytotoxic activity of novel protoflavone analogs – selectivity towards a multidrug resistant cancer cell line.

  • Autores: Amaral L, Chang FR, Chuang DW, Danko B, Hunyadi A, Martins A, Molnar J, Wang HC, Wu YC
  • Ano de Publicação: 2012
  • Journal: Anticancer Research
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=In+vitro+cytotoxic+activity+of+novel+protoflavone+analogs+%E2%80%93selectivity+towards+a+multidrug+resistant+cancer+cell+line

BACKGROUND:
Protoapigenone (PA), a natural flavonoid possessing an unusual p-quinol moiety on its B ring, is a prospective novel lead compound against cancer currently in development, together with WYC0209, a potent synthetic PA analog. Structure activity relationships (SAR) concerning different 1′-O-alkyl side-chains were also studied on two sets of derivatives.
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Inhibitors of bacterial efflux pumps that also inhibit efflux pumps of cancer cells.

  • Autores: Amaral L, Armada A, Handzlik J, Kiec-Kononowicz K, Martins A, Molnar J, Spengler G
  • Ano de Publicação: 2012
  • Journal: Anticancer Research
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/22753759

Bacteria and cancer cells frequently increase their resistance to chemotherapeutics as a consequence of therapy. Whenever studied, refractory response to chemotherapy is due to the over-expression of efflux pumps that render the bacterium or cancer cell resistant not only to the agent used for therapy, but to many, if not all other agents as well.
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