Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs

Ajay Kumar; Bhahwal A Shah; Samar Singh; Abid Hamid; Shashank K Singh; Vijay K Sethi; Ajit K Saxena; Jaswant Singh; Subhash C Taneja

doi:10.1016/j.bmcl.2011.10.112

Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs

Bioorg Med Chem Lett. 2012 Jan 1;22(1):431-5. doi: 10.1016/j.bmcl.2011.10.112. Epub 2011 Nov 9.

Authors

Ajay Kumar¹, Bhahwal A Shah, Samar Singh, Abid Hamid, Shashank K Singh, Vijay K Sethi, Ajit K Saxena, Jaswant Singh, Subhash C Taneja

Affiliation

¹ Natural Product Microbes Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu Tawi 180 001, India.

PMID: 22123322
DOI: 10.1016/j.bmcl.2011.10.112

Abstract

Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to the development of a possible SAR. One of the identified lead compounds was found to be an inhibitor of the NF-κB and STAT proteins, warranting further investigations to be developed into a potential anticancer lead.

MeSH terms

Antineoplastic Agents / pharmacology
Cell Line, Tumor
Cell Proliferation
Drug Design
Drug Screening Assays, Antitumor / methods
Flow Cytometry / methods
HL-60 Cells
Humans
Models, Chemical
NF-kappa B / metabolism*
Phosphorylation
STAT Transcription Factors / metabolism*
Triterpenes / chemistry
Triterpenes / pharmacology*

Substances

Antineoplastic Agents
NF-kappa B
STAT Transcription Factors
Triterpenes
boswellic acid