Planta Med 2015; 81 - PK8
DOI: 10.1055/s-0035-1556286

Discovery of novel bioactive natural product-like compounds based on diversity-enhanced reactions

Y Guan 1, 2, J Wang 1, H Zhang 1
  • 1School of Chinese Medicine, Hong Kong Baptist University, Hong Kong SAR, P. R. China
  • 2HKBU Shenzhen Research Center, Shenzhen, P. R. China

Diversity-enhanced reaction (DER), a non-selectivity and non-specificity reaction, is proposed to increase the diversified chemical structures of natural products for drug discovery (Fig. 1). We have applied this method to quickly synthesize a number of BB1608-like derivatives (Scheme 1). 2 underwent DER to afford a mixture. Separation and derivatization provided 3 – 12, Compounds 3 – 12 were evaluated for their anticancer and antiviral activities. The development of more complex DER is in progress. [The work described in this paper was supported by HKBU Interdisciplinary Research Matching Scheme (RC-IRMS/12 – 13/03) and Natural Science Foundation of China (No. 21402166)].

Fig. 1: Diversity-enhanced reaction-a new approach of synthesis of structural diversity of natural product-like

Scheme 1: Synthesis of BB1608-like compounds by diversity-enhanced reaction