63792-75-6Relevant academic research and scientific papers
Comprehensive study of sansalvamide A derivatives and their structure-activity relationships against drug-resistant colon cancer cell lines
Otrubova, Katerina,Lushington, Gerald,Vander Velde, David,McGuire, Kathleen L.,McAlpine, Shelli R.
, p. 530 - 544 (2008/09/18)
We report an extensive structure-activity relationship (SAR) of 62 compounds active against two drug-resistant colon cancer cell lines. Our comprehensive evaluation of two generations of compounds utilizes SAR, NMR, and molecular modeling to evaluate the
Synthesis and cytotoxicity of a new class of potent decapeptide macrocycles
Davis, Melinda R.,Styers, Thomas J.,Rodriguez, Rodrigo A.,Pan, Po-Shen,Vasko, Robert C.,McAlpine, Shelli R.
, p. 177 - 180 (2008/09/19)
(Chemical Equation Presented) Described are the syntheses of five decapeptides that are C-2-symmetrical derivatives of the natural product pentapeptide sansalvamide A. Derivatives were made using a succinct convergent synthesis. These analogues share no s
Synthesis of second-generation Sansalvamide A derivatives: Novel templates as potential antitumor agents
Rodriguez, Rodrigo A.,Pan, Po-Shen,Pan, Chung-Mao,Ravula, Suchitra,Lapera, Stephanie,Singh, Erinprit K.,Styers, Thomas J.,Brown, Joseph D.,Cajica, Julia,Parry, Emily,Otrubova, Katerina,McAlpine, Shelli R.
, p. 1980 - 2002 (2007/10/03)
We report the synthesis of 34 second-generation Sansalvamide A derivatives. San A derivatives have unique anticancer properties and target multiple cancers, including colon, pancreatic, breast, prostate, and melanoma. As novel templates, the derivatives d
Synthesis of Sansalvamide A derivatives and their cytotoxicity in the MSS colon cancer cell line HT-29
Styers, Thomas J.,Kekec, Ahmet,Rodriguez, Rodrigo,Brown, Joseph D.,Cajica, Julia,Pan, Po-Shen,Parry, Emily,Carroll, Chris L.,Medina, Irene,Corral, Ricardo,Lapera, Stephanie,Otrubova, Katerina,Pan, Chung-Mao,McGuire, Kathleen L.,McAlpine, Shelli R.
, p. 5625 - 5631 (2007/10/03)
We report the synthesis of thirty-six Sansalvamide A derivatives, and their biological activity against colon cancer HT-29 cell line, a microsatellite stable (MSS) colon cancer cell-line. The thirty-six compounds can be divided into three subsets, where t
High-yielding macrocyclization conditions used in the synthesis of novel Sansalvamide A derivatives
Styers, Thomas J.,Rodriguez, Rodrigo,Pan, Po-Shen,McAlpine, Shelli R.
, p. 515 - 517 (2007/10/03)
Described are the syntheses of nine Sansalvamide A derivatives using new, high-yielding, in situ deprotection-cyclization conditions that are general for this series of macrocycles, 55% average for both steps. This is 10-fold greater than previously repor
Conformational aspects of human formylpeptide receptor antagonists
Scatturin, Angelo,Vertuani, Gianni,Pecoraro, Rita,Dalpiaz, Alessandro,Boggian, Marisa,Ferretti, Maria Enrica,Spisani, Susanna
, p. 873 - 877 (2007/10/03)
The conformation of several Phe-D-Leu-Phe-D-Leu-Phe analogues was analyzed using infrared absorption and circular dichroism. Their effect on human neutrophils was verified by receptor binding and chemotaxis assays. The results demonstrate that the compounds examined prefer an ordered conformation (β-turn) in amphipatic environment, and that they are able to antagonize the neutrophil functions evoked by CHO-Met-Leu-Phe.
