132994-16-2

Upstream product

• 5693-62-9 2,3,4,5-tetrahydro-6-methoxypyridine 

Downstream Products

• 676334-81-9 4-(4-phenethylpiperazin-1-yl)-6,7,8,9-tetrahydropyrimido[4,5-b]-indolizine-10-carbonitrile 
• 676334-94-4 4-{4-[2-(3-nitro-phenyl)-ethyl]-piperazin-1-yl}-5,6,7,8-tetrahydro-1,3,4b-triaza-fluorene-9-carbonitrile 
• 676335-00-5 4-{4-[2-(3,4-difluoro-phenyl)-ethyl]-piperazin-1-yl}-5,6,7,8-tetrahydro-1,3,4b-triaza-fluorene-9-carbonitrile 
• 731824-15-0 4-(4-phenylpiperazin-1-yl)-6,7,8,9-tetrahydropyrimido[4,5-b]-indolizine-10-carbonitrile 

Relevant academic research and scientific papers

Pyrrolopyrimidine Derivatives as Novel Inhibitors of Multidrug Resistance-Associated Protein 1 (MRP1, ABCC1)

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).