- CYCLIC PEPTIDE ANTITUMOR AGENTS
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Cyclic peptide compounds and derivatives thereof having antitumor activity as shown by treatment of human melanoma, pancreatic, breast, prostate cancer cells.
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Page/Page column 11-12; 15
(2010/02/11)
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- N-methylsansalvamide a peptide analogues. Potent new antitumor agents
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Sansalvamide A, a cyclic depsipeptide isolated from a marine fungus of the genus Fusarium, is composed of four hydrophobic amino acids (Phe, two Leu, Val) and one hydroxy acid ((S)-2-hydroxy-4-methylpentanoic acid; O-Leu) with five stereogenic centers all having S-stereochemistry. We have recently synthesized the corresponding cyclic peptide (Gu, W.; Liu, S.; Silverman, R. B. Organic Lett. 2002, 4, 4171-4174) and found that it too has antitumor activity. N-Methylation can enhance potency and selectivity for peptides. Consequently, here we synthesize 12 different N-methylated sansalvamide A peptide analogues and show that for several different tumor cell lines three of these analogues are more potent than the natural product; in pancreatic cells, sansalvamide A shows little activity, but the N-methylsansalvamide peptides are potent cytotoxic agents.
- Liu, Shouxin,Gu, Wenxin,Lo, Denise,Ding, Xian-Zhong,Ujiki, Michael,Adrian, Thomas E.,Soff, Gerald A.,Silverman, Richard B.
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p. 3630 - 3638
(2007/10/03)
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