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Antimalarial Agents, 4. Synthesis of a Brusatol Analog and Biological Activity of Brusatol-Related Compounds

K H Lee, S Tani, Y Imakura

J Nat Prod. Sep-Oct 1987;50(5):847-51.

PMID: 3325613

Abstract:

The quassinoids bruceoside-A [1], brusatol [2], and bruceolide [3] were tested for antimalarial activity in vitro against the chloroquine-resistant (Smith) isolates of Plasmodium falciparum. Compound 2 was quite active, 1 was not active, and 3 showed only a trace of activity. The fact that 15 [(E)-non-2-enoyl] bruceolide [7] synthesized from 2 was eight times less active than 2 would indicate that the requirement of a C-15 ester moiety for enhanced antimalarial activity among brusatol related quassinoids could be quite specific.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
ALP5428615 Chloroquine Related Compound E Chloroquine Related Compound E 5428-61-5 (free base) Price
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