Cribrostatins 1 and 2

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

IPC codes

C07D 217/24 (2006.01) A61K 31/47 (2006.01)

Type

Patent

Patent number

CA 2074701

Description

ABSTRACT OF THE DISCLOSURE The blue marine sponge Cribrochalina sp., collected in the Republic of the Maldives, was found to contain the new cell growth inhibitory isoquinolinequinones designated cribrostatin 1 (8.8 x 10-6% yield) and 2 (3.1 x 1016% yield) which are active against the P388 lymphocytic leukemia cell line (PS ED50 1.58 µg/mL, PS ED50 2.73 µg/mL, respectively). Importantly, both cribrostatins 1 and 2 have shown selective activity against all of the nine human melanoma cell lines employed by the U.S. National Cancer Institute. Structural determinations of both substances were accomplished utilizing high field NMR (400 MHz) and mass spectral studies. Confirmation of the cribrostatin 1 structure was achieved by X-ray crystallographic techniques. -17-

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