A bifunctional dimethylsulfoxide substitute enhances the aqueous solubility of small organic molecules

Assay Drug Dev Technol. 2012 Jun;10(3):269-77. doi: 10.1089/adt.2011.0421. Epub 2011 Dec 22.

Abstract

An oxetane-substituted sulfoxide has demonstrated potential as a dimethylsulfoxide substitute for enhancing the dissolution of organic compounds with poor aqueous solubilities. This sulfoxide may find utility in applications of library storage and biological assays. For the model compounds studied, significant solubility enhancements were observed using the sulfoxide as a cosolvent in aqueous media. Brine shrimp, breast cancer (MDA-MB-231), and liver cell line (HepG2) toxicity data for the new additive are also presented, in addition to comparative IC(50) values for a series of PKD1 inhibitors.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cell Line
  • Dimethyl Sulfoxide / chemistry*
  • Dimethyl Sulfoxide / toxicity
  • Humans
  • Liver / drug effects
  • Organic Chemicals / chemistry*
  • Organic Chemicals / toxicity
  • Solubility
  • Solvents / chemistry
  • Solvents / toxicity
  • Water / chemistry*

Substances

  • Organic Chemicals
  • Solvents
  • Water
  • Dimethyl Sulfoxide