Epothilone D and its 9-Methyl analogues: combinatorial syntheses, conformation, and biological activities

Eur J Med Chem. 2013 Oct:68:321-32. doi: 10.1016/j.ejmech.2013.08.003.

Feng Sang ¹, Peng Feng, Jie Chen, Yahui Ding, Xiyan Duan, Jiadai Zhai, Xiaoyan Ma, Bin Zhang, Quan Zhang, Jianping Lin, Yue Chen

Affiliations

Affiliation

1 State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Nankai University, Tianjin 300071, PR China.

PMID: 23994325 DOI: 10.1016/j.ejmech.2013.08.003

Abstract

Epothilone D (Epo D) and its 9-Methyl conformational analogues were synthesized through a highly efficient combinatorial approach. The fragment E was synthesized in 11 total steps with 6 longest linear steps, and each aldehyde B was prepared via a 3-step sequence. Starting from the common precursor E and a suitable aldehydes B, each target molecule were obtained in only 4 steps. The 9-(S)-epo D and 9-(R)-epo D demonstrated significant difference in inhibition activities against Cancer cell lines and in conformational analysis.

Keywords

Analogues; Bioactivity; Epothilone; Structure activity relationship; Total synthesis.

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