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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis of A/B-Ring Partial Analogs of Bruceantin as Potential Antimalarial Agents

Author(s): Z. Guo, S. Vangapandu, A. Nimrod, L. A. Walker and R. D. Sindelar

Volume 1 , Issue 1 , 2005

Page: [3 - 11] Pages: 9

DOI: 10.2174/1573406053402488

Abstract

Bruceantin (1), a classical quassinoid with the highest reported antimalarial activity among the quassinoids examined thus far, was selected as a natural product lead for the design of a series of A/B-ring analogs. A viable strategy for the synthesis of the series was developed. The functionalized A-ring and the C-15 ester moiety in bruceantin are incorporated in all designed compounds. The preliminary bioassay results will be discussed in detail.

Keywords: bruceantin, partial analogs, bioassay, structure activity relationships, antileukemic and antimalarial activities


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