Synthesis and cytotoxic activity of some novel steroidal C-17 pyrazolinyl derivatives

  • Eur J Med Chem. 2013 Nov:69:182-90. doi: 10.1016/j.ejmech.2013.08.016.
Ning-Juan Fan  1 ,  Jiang-Jiang Tang ,  He Li ,  Xiao-Jun Li ,  Bo Luo ,  Jin-Ming Gao
Affiliations
  • 1. Shaanxi Engineering Center of Bioresource Chemistry & Sustainable Utilization, College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China.
PMID: 24021891 DOI: 10.1016/j.ejmech.2013.08.016
Abstract

Fourteen novel steroidal C-17 pyrazolinyl derivatives 9a-g and 10a-g were synthesized from commercially available progesterone and tested for their cytotoxic activity against brine shrimp (Artemia salina) and three human Cancer cell lines (NCI-H460, HeLa, and HepG2). Some of these synthetic compounds exhibited significant cytotoxic activity, and treatment of HeLa cells with compound 10b resulted in the cell population arrest in the S phase. A structure-activity relationship was discussed.

Keywords
Cytotoxicity; Progesterone; Pyrazoline; Steroid; Steroidal heterocycles.