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Semisynthesis and Cytotoxicity of Hypothemycin Analogues
Author(s) -
Hearn Brian R.,
Sundermann Kurt,
Cannoy Jonah,
Santi Daniel V.
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700128
Subject(s) - semisynthesis , cytotoxicity , chemistry , stereochemistry , computer science , combinatorial chemistry , world wide web , biochemistry , in vitro
Evaluation of the hypothemycin cytotoxicity SAR identifies the C4′–C8′ region of the macrocyclic lactone as relatively intolerant of structural modifications. Manipulation of the 4‐position of the resorcylic acid, however, provides new opportunities to improve solubility and pharmacokinetic properties as this site may be modified without negatively impacting cytotoxicity.