2. Academic Validation
  3. Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives

Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5058-62. doi: 10.1016/j.bmcl.2008.08.003.
Vivek Kumar 1,  Nidhi Rani,  Pawan Aggarwal,  Vinod K Sanna,  Anu T Singh,  Manu Jaggi,  Narendra Joshi,  Pramod K Sharma,  Raghuveer Irchhaiya,  Anand C Burman
Affiliations

Affiliation

  • 1 Chemical Research, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201010, UP, India. kumarv@dabur.com
PMID: 18752941 DOI: 10.1016/j.bmcl.2008.08.003
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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