1267947-19-2Relevant academic research and scientific papers
Chemical synthesis and biological evaluation of second-generation palmerolide a analogues
Ravu, Vengala Rao,Leung, Gulice Y. C.,Lim, Chek Shik,Ng, Sin Yee,Sum, Rong Ji,Chen, David Y.-K.
supporting information; experimental part, p. 463 - 468 (2011/04/17)
In this communication, second-generation analogues of palmerolide A, a recently reported cytotoxic agent against melanoma cancer cells, were rationally designed, synthesized, and biologically evaluated. Structural variations of the enamide side chain and the C1-C8 segment of palmerolide A revealed a narrow structure-activity relationship window of the newly synthesized compounds. In addition, mechanistic and pharmacological studies were performed to assess the therapeutic potential of palmerolide A. Synthesis and biological evaluation of second-generation palmerolide A analogues are reported. This study focused on further modification of the enamide side chain, and the C1-C8 carbon backbone of palmerolide A. Structure-activity relationship, mechanistic, and pharmacological investigations of the palmerolide compounds pave the foundation for the ensuing in vivo studies.
