Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives |
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Authors: | Kumar Vivek Rani Nidhi Aggarwal Pawan Sanna Vinod K Singh Anu T Jaggi Manu Joshi Narendra Sharma Pramod K Irchhaiya Raghuveer Burman Anand C |
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Institution: | Chemical Research, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201010, UP, India. kumarv@dabur.com |
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Abstract: | A new series of betulinic acid derivatives have been synthesized by introducing heterocyclic ring between C-2 and C-3 positions of betulinic acid. Further modifications were also carried out by reduction of C-20(29) unsaturated bond and substitution of C-28 carboxyl group by ester and amide linkage to enhance the selectivity. Compound 11 resulted in IC(50) of 2.44, 2.5, and 2.7 microg/ml on MIAPaCa, PA-1, and SW620 cancer cell lines, respectively. Compound 38 resulted in IC(50) of 0.67 microg/ml on MIAPaCa cell line. |
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