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Mar. Drugs 2014, 12(6), 3574-3586; doi:10.3390/md12063574

Diazaquinomycins E–G, Novel Diaza-Anthracene Analogs from a Marine-Derived Streptomyces sp.

1
Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, IL 60612, USA
2
Center for Pharmaceutical Biotechnology, University of Illinois at Chicago, Chicago, IL 60607, USA
*
Author to whom correspondence should be addressed.
Received: 12 May 2014 / Revised: 25 May 2014 / Accepted: 28 May 2014 / Published: 11 June 2014
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Abstract

As part of our program to identify novel secondary metabolites that target drug-resistant ovarian cancers, a screening of our aquatic-derived actinomycete fraction library against a cisplatin-resistant ovarian cancer cell line (OVCAR5) led to the isolation of novel diaza-anthracene antibiotic diazaquinomycin E (DAQE; 1), the isomeric mixture of diazaquinomycin F (DAQF; 2) and diazaquinomycin G (DAQG; 3), and known analog diazaquinomycin A (DAQA; 4). The structures of DAQF and DAQG were solved through deconvolution of X-Ray diffraction data of their corresponding co-crystal. DAQE and DAQA exhibited moderate LC50 values against OVCAR5 of 9.0 and 8.8 μM, respectively. At lethal concentrations of DAQA, evidence of DNA damage was observed via induction of apoptosis through cleaved-PARP. Herein, we will discuss the isolation, structure elucidation, and biological activity of these secondary metabolites. View Full-Text
Keywords: actinomycete; marine; Streptomyces; ovarian cancer; OVCAR5; diazaquinomycin actinomycete; marine; Streptomyces; ovarian cancer; OVCAR5; diazaquinomycin
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MDPI and ACS Style

Mullowney, M.W.; Ó hAinmhire, E.; Shaikh, A.; Wei, X.; Tanouye, U.; Santarsiero, B.D.; Burdette, J.E.; Murphy, B.T. Diazaquinomycins E–G, Novel Diaza-Anthracene Analogs from a Marine-Derived Streptomyces sp.. Mar. Drugs 2014, 12, 3574-3586.

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