Search Results - "Singh, Erinprit K"
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Synthesis of sansalvamide A peptidomimetics: triazole, oxazole, thiazole, and pseudoproline containing compounds
Published in Tetrahedron (28-01-2012)“…Peptidomimetic-based macrocycles typically have improved pharmacokinetic properties over those observed with peptide analogs. Described are the syntheses of 13…”
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Journal Article -
2
Macrocyclic inhibitors of hsp90
Published in Current topics in medicinal chemistry (01-10-2010)“…Heat shock proteins (HSP) are a family of highly conserved proteins, whose expression increases in response to stresses that may threaten cell survival. Over…”
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Journal Article -
3
Synthesis of Second-Generation Sansalvamide A Derivatives: Novel Templates as Potential Antitumor Agents
Published in Journal of organic chemistry (16-03-2007)“…We report the synthesis of 34 second-generation Sansalvamide A derivatives. San A derivatives have unique anticancer properties and target multiple cancers,…”
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Journal Article -
4
Total Synthesis of trans,trans-Sanguinamide B and Conformational Isomers
Published in Organic letters (02-03-2012)“…The first total synthesis of Sanguinamide B is reported, prepared via an efficient synthetic strategy. The natural product, trans,trans-Sanguinamide B (1), was…”
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Journal Article -
5
Synthesis, Structure–Activity Analysis, and Biological Evaluation of Sanguinamide B Analogues
Published in Journal of organic chemistry (07-12-2012)“…We report the first synthesis of sanguinamide B analogues. Substituting N-methylated (N-Me) amino acids, glycine (Gly), and l- or d-phenylalanine (Phe) into…”
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Journal Article -
6
Design and synthesis of Hsp90 inhibitors: Exploring the SAR of Sansalvamide A derivatives
Published in Bioorganic & medicinal chemistry (15-09-2010)“…Utilizing the structure–activity relationship we have developed during the synthesis of the first two generations and mechanism of action studies that point to…”
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Journal Article -
7
Histone deacetylase inhibitors: synthesis of cyclic tetrapeptides and their triazole analogs
Published in Tetrahedron letters (18-08-2010)“…Synthesis of nine macrocyclic peptide HDAC inhibitors and three triazole derivatives is described. HDAC inhibitory activity of these compounds against HeLa…”
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Journal Article -
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Synthesis and biological evaluation of histone deacetylase inhibitors that are based on FR235222: A cyclic tetrapeptide scaffold
Published in Bioorganic & medicinal chemistry (15-04-2008)“…We outline the synthesis of six novel derivatives that are based on a recently discovered HDAC inhibitor FR235222. Our work is the first report utilizing a…”
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Journal Article -
9
Conformationally based design of macrocycles as antitumor agents
Published in Current opinion in drug discovery & development (01-07-2008)“…A key feature for any chemotherapeutic agent is a favorable conformation when it is presenting itself to its intended target. Numerous macrocycles have been…”
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Journal Article -
10
Design and synthesis of bioactive macrocyclic natural products
Published 01-01-2012“…Chapter 1 discusses the background of peptides and their potential as therapeutics; specifically as anti-cancer and antibacterial agents. The synthesis of…”
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Dissertation -
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Design and synthesis of bioactive macrocyclic natural products
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Dissertation