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- W2292943446 abstract "Five series of pyrrolo[3,2-d]pyrimidines were synthesized and evaluated with respect to potency and selectivity toward multidrug resistance-associated protein 1 (MRP1, ABCC1). This transport protein is a major target to overcome multidrug resistance in cancer patients. We investigated differently substituted pyrrolopyrimidines using the doxorubicin selected and MRP1 overexpressing small cell lung cancer cell line H69 AR in a calcein AM and daunorubicin cell accumulation assay. New compounds with high potency and selectivity were identified. Piperazine residues at position 4 bearing large phenylalkyl side chains proved to be beneficial for MRP1 inhibition. Its replacement by an amino group led to decreased activity. Aliphatic and aliphatic–aromatic variations at position 5 and 6 revealed compounds with IC50 values in high nanomolar range. All investigated compounds had low affinity toward P-glycoprotein (P-gp, ABCB1). Pyrrolopyrimidines with small substituents showed moderate inhibition against breast cancer resistance protein (BCRP, ABCG2)." @default.
- W2292943446 created "2016-06-24" @default.
- W2292943446 creator A5009888182 @default.
- W2292943446 creator A5041659266 @default.
- W2292943446 creator A5052330076 @default.
- W2292943446 date "2016-03-17" @default.
- W2292943446 modified "2023-10-18" @default.
- W2292943446 title "Pyrrolopyrimidine Derivatives as Novel Inhibitors of Multidrug Resistance-Associated Protein 1 (MRP1, ABCC1)" @default.
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- W2292943446 doi "https://doi.org/10.1021/acs.jmedchem.5b01644" @default.
- W2292943446 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26943020" @default.
- W2292943446 hasPublicationYear "2016" @default.
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