2. Academic Validation
  3. Sterols as anticancer agents: synthesis of ring-B oxygenated steroids, cytotoxic profile, and comprehensive SAR analysis

Sterols as anticancer agents: synthesis of ring-B oxygenated steroids, cytotoxic profile, and comprehensive SAR analysis

  • J Med Chem. 2010 Nov 11;53(21):7632-8. doi: 10.1021/jm1007769.
João F S Carvalho 1,  M Manuel Cruz Silva,  João N Moreira,  Sérgio Simões,  M Luisa Sá e Melo
Affiliations

Affiliation

  • 1 Center for Pharmaceutical Studies, University of Coimbra, Portugal.
PMID: 20931970 DOI: 10.1021/jm1007769
Abstract

The cytotoxicity of oxysterols was systematically studied in tumor and normal cells. Synthetic strategies to prepare this library included oxidations at ring B and a new method to yield 6β-hemiphthalates directly from Δ(5)-steroids. Most oxysterols were cytotoxic and showed selectivity toward Cancer cells, LAMA-84 cells (leukemia) being particularly sensitive to 4, 8, 22, and 27 (IC(50) < 5.6 μM). The structural requirements to induce selective toxicity are discussed to shed light on the development of new Anticancer drugs.

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