Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 4, Pages 1342-1354Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.12.067
Keywords
Neolignans; Lignans; Anticancer; Microtubules; In silico studies; Acute oral toxicity
Funding
- SIP [BSC203]
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Tubulin is a well established target for anticancer drug development. Lignans and neolignans were synthesized as tubulin interacting agents. Neolignans 10 and 19 exhibited significant anticancer activity against MCF-7 and MDAMB-231 human breast cancer cell lines. Both the compounds effectively induced stabilization of microtubule at 4 and 20 mu M concentrations respectively. Neolignan 10 induced G2/M phase arrest in MCF-7 cells. Docking experiments raveled that 10 and 19 occupied the same binding pocket of paclitaxel with some difference in active site amino acids and good bioavailability of both the compounds. In in vivo acute oral toxicity 10 was well tolerated up to 300 mg/kg dose in Swiss-albino mice. (C) 2014 Elsevier Ltd. All rights reserved.
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