12 research outputs found

    HCC patient voices survey

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    Background: Hepatocellular carcinoma (HCC) is the sixth most commonly-diagnosed cancer globally, and the second-leading cause of cancer deaths annually. To better understand the patient journey we conducted the first global survey of patients with HCC in 13 countries.The survey was live from November 2016 to April 2017 and gathered data from 256 respondents

    A new class of 1-aryl-5,6-dihydropyrrolo[2,1-a]isoquinoline derivatives as reversers of P-glycoprotein-mediated multidrug resistance in tumor cells

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    A number of aza-heterocyclic compounds, which share with members of the lamellarin alkaloids' family the 5,6-dihydropyrrolo[2,1-a]isoquinoline (DHPIQ) scaffold, were synthesized and evaluated for their ability to reverse in vitro multidrug resistance (MDR) in cancer cells, through inhibition of P-glycoprotein (P-gp) and/or multidrug-resistance-associated protein-1 (MRP-1). Most of the investigated DHPIQs proved to be selective P-gp modulators, and the most potent ones, which are 2-carbaldehydes (3 and 4) or a thiosemicarbazone derivative (10), attained submicromolar inhibition potencies (average IC50s of 0.24, 0.19 and 0.24 µM, respectively). Schiff bases prepared by condensation of some 1-aryl-DHPIQ aldehydes with p-aminophenol also proved to be of some interest, compound 15 displaying IC50 of 1.01 µM. In drug combination assays in multidrug-resistant cells, some DHPIQ compounds, at non-toxic doses, significantly increased the cytotoxicity of doxorubicin in a concentration-dependent manner. Structure-activity relationship studies and investigation of the chemical stability of the Schiff bases provided physicochemical information useful for molecular optimization of lamellarin-like cytotoxic drugs active toward chemoresistant tumors as well as non-toxic reversers of P-gp-mediated MDR in tumor cells
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