Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.

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O'Connell CE, Salvato KA, Meng Z, Littlefield BA, Schwartz CE

Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1541-6.

PubMed ID

10386932 [ View in PubMed

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Abstract

The marine natural product hapalosin and 22 analogs, which incorporated systematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and general cytotoxicity. Some substituent modifications resulted in lower cytotoxicities, but most structural changes were either detrimental to or did not seriously alter the MDR-reversing activity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Verapamil	P-glycoprotein 1	IC 50 (nM)	3100	N/A	N/A	Details
Verapamil	P-glycoprotein 1	IC 50 (nM)	53000	N/A	N/A	Details