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Synthesis of Simplified Tedanolide Analogues—Connecting Tedanolide to Myriaporone and Gephyronic Acid
Author(s) -
Diaz Nina,
Naini Arun,
Muthukumar Yazh,
Sasse Florenz,
Kalesse Markus
Publication year - 2012
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.201100576
Subject(s) - potency , natural product , in vitro , chemistry , cell culture , stereochemistry , cancer cell lines , combinatorial chemistry , structure–activity relationship , computational biology , biochemistry , pharmacology , cancer cell , cancer , biology , genetics
Southern belles! Simplified analogues of tedanolide, a natural product with picomolar activity against a range of tumor cell lines, were synthesized and evaluated for potency in mammalian cancer cells. The truncated analogues were found to retain significant activity in vitro (23 μmol mL −1 for the example shown) compared with the parent compound tedanolide (0.33 nmol mL −1 ), and represent potential leads for the development of novel anticancer agents.