Kumar Vivek, Rani Nidhi, Aggarwal Pawan, Sanna Vinod K, Singh Anu T, Jaggi Manu, Joshi Narendra, Sharma Pramod K, Irchhaiya Raghuveer, Burman Anand C
Chemical Research, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201010, UP, India.
Bioorg Med Chem Lett. 2008 Sep 15;18(18):5058-62. doi: 10.1016/j.bmcl.2008.08.003. Epub 2008 Aug 6.
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.
通过在桦木酸的C-2和C-3位之间引入杂环，合成了一系列新的桦木酸衍生物。还通过还原C-20(29)不饱和键以及用酯和酰胺键取代C-28羧基进行了进一步修饰，以提高选择性。化合物11在MIAPaCa、PA-1和SW620癌细胞系上的IC(50)分别为2.44、2.5和2.7微克/毫升。化合物38在MIAPaCa细胞系上的IC(50)为0.67微克/毫升。
