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Issue 1, 2015
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Synthesis, structure–activity relationship, and mechanistic investigation of lithocholic acid amphiphiles for colon cancer therapy

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Abstract

We report a structure–activity relationship of lithocholic acid amphiphiles for their anticancer activities against colon cancer. We synthesized ten cationic amphiphiles, differing in nature of their cationic charged head groups, using lithocholic acid. We observed that anticancer activities of these amphiphiles against colon cancer cell lines are contingent on nature of the charged head group. The lithocholic acid-based amphiphile possessing a piperidine head group (LCA-PIP1) is ∼10 times more cytotoxic than its precursor. Biochemical studies revealed that enhanced activity of LCA-PIP1 compared to lithocholic acid is due to a greater activation of apoptosis. LCA-PIP1 induces sub G0 arrest and causes cleavage of caspases. A single dose of lithocholic acidpiperidine (LCA-PIP1) derivative is enough to reduce the tumor burden by 75% in a tumor xenograft model.

Graphical abstract: Synthesis, structure–activity relationship, and mechanistic investigation of lithocholic acid amphiphiles for colon cancer therapy

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Publication details

The article was received on 28 May 2014, accepted on 14 Oct 2014 and first published on 15 Oct 2014


Article type: Concise Article
DOI: 10.1039/C4MD00223G
Citation: Med. Chem. Commun., 2015,6, 192-201
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    Synthesis, structure–activity relationship, and mechanistic investigation of lithocholic acid amphiphiles for colon cancer therapy

    M. Singh, S. Bansal, S. Kundu, P. Bhargava, A. Singh, R. K. Motiani, R. Shyam, V. Sreekanth, S. Sengupta and A. Bajaj, Med. Chem. Commun., 2015, 6, 192
    DOI: 10.1039/C4MD00223G

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