2. Academic Validation
  3. SPF32629A and SPF32629B: enantioselective synthesis, determination of absolute configuration, cytotoxicity and antibacterial evaluation

SPF32629A and SPF32629B: enantioselective synthesis, determination of absolute configuration, cytotoxicity and antibacterial evaluation

  • Eur J Med Chem. 2011 May;46(5):1803-12. doi: 10.1016/j.ejmech.2011.02.039.
Srinivasa Rao Vegi 1,  Shanthaveerappa K Boovanahalli,  Balaram Patro,  K Mukkanti
Affiliations

Affiliation

  • 1 Medicinal Chemistry Laboratory, GVK Biosciences Private Limited, Plot No.28, IDA, Nacharam, Hyderabad 500 076, AP, India.
PMID: 21397370 DOI: 10.1016/j.ejmech.2011.02.039
Abstract

We report herein an efficient enantioselective synthesis of SPF32629A and SPF32629B through one-pot enantioselective reduction and protecting-group-free regioselective O-acylation strategy. The absolute configuration of the enantiomerically pure isomers was established by Mosher ester analysis. The inhibitory potencies of the synthesized compounds were assayed in vitro against a panel of Microorganisms and against A549 human lung adenocarcinoma cell line. Compounds 2, 11 and 12 displayed moderate to potent Antibacterial activity against all the tested strains and compounds 7, 8, 2, 11 and 12 exhibited significant cytotoxicity in a dose-dependent manner with an IC50 values ranging from 2.92 to 4.14 μg/ml and 8-11 μM.

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