Synthesis and biological evaluation of 12-, 13-, 14-membered macrolides and open chain 2,6-trans-disubstituted dihydropyran analogues for aspergillides |
| |
| Authors: | Srihari Pabbaraja Naresh Gantasala Sridhar Ydhyam Hari Krishna Namballa Subhashini Gundeboina Mallikharjuna R Lambu Sanjeev Meena Dipak Datta |
| |
| Institution: | 1. Department of Organic Synthesis & Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;2. Academy of Scientific and innovative Research (AcSIR), Anusandhan Bhawan, 2-Rafi Marg, NewDelhi 110001, India;3. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500037, India;4. Biochemistry Division, Council of Scientific & Industrial Research (CSIR), Central Drug Research Institute (CDRI), Lucknow, India |
| |
| Abstract: | Stereoselective synthesis of twenty (three 12-, five 13- and twelve 14-membered) macrolides and seventeen functionalized 2,6-trans-disubstituted dihydropyran derivatives have been achieved. The key reactions include an Achmatowicz rearrangement, Ferrier-type alkynylation, Yamaguchi macrolactonization and Lindlar’s hydrogenation. Biological screening of the synthesised compounds showed moderate activity against human cancer cell-lines. |
| |
| Keywords: | Aspergillides Macrolides Cancer Ferrier Achmatowicz |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
