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Rare Streptomyces N-formyl amino-salicylamides inhibit oncogenic K-Ras.

Organic letters (2014-09-23)
Angela A Salim, Kwang-Jin Cho, Lingxiao Tan, Michelle Quezada, Ernest Lacey, John F Hancock, Robert J Capon
ABSTRACT

During a search for inhibitors of oncogenic K-Ras, we detected two known and two new examples of the rare neoantimycin structure class from a liquid cultivation of Streptomyces orinoci, and reassigned/assigned structures to all based on detailed spectroscopic analysis and microscale C3 Marfey's and C3 Mosher chemical degradation/derivatization/analysis. SAR investigations inclusive of the biosynthetically related antimycins and respirantin, and synthetic benzoxazolone, documented a unique N-formyl amino-salicylamide pharmacophore as a potent inhibitor of oncogenic K-Ras.

MATERIALS
Product Number
Brand
Product Description

Doxorubicin hydrochloride, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Doxorubicin hydrochloride, 98.0-102.0% (HPLC)
Sigma-Aldrich
Doxorubicin hydrochloride, suitable for fluorescence, 98.0-102.0% (HPLC)