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

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.

SUBMITTER: Salim AA

PROVIDER: S-EPMC5645021 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature

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

Salim Angela A AA Cho Kwang-Jin KJ Tan Lingxiao L Quezada Michelle M Lacey Ernest E Hancock John F JF Capon Robert J RJ

Organic letters 20140919 19

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-form ...[more]

PMID: 25238489

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