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Editorial

Is there enough focus on lipophilicity in drug discovery?

Pages 261-263 | Received 06 Sep 2019, Accepted 08 Nov 2019, Published online: 17 Nov 2019

References

  • DiMasi JA, Grabowski HG, Hansen RW. Innovation in the pharmaceutical industry: new estimates of r&d costs. J Health Econ. 2016;47:20–33.
  • Lipinski CA, Lombardo F, Dominy BW, et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 2001;46(1–3):3–26.
  • Giaginis C, Tsopelas F, Tsantili-Kakoulidou A. The impact of lipophilicity in drug discovery: rapid measurements by means of reversed-phase hplc. Methods Mol Biol. 2018;1824:217–228.
  • Tsopelas F, Giaginis C, Tsantili-Kakoulidou A. Lipophilicity and biomimetic properties to support drug discovery. Expert Opin Drug Discov. 2017;12(9):885–896.
  • Leeson PD, St-Gallay SA. The influence of the ‘organizational factor’ on compound quality in drug discovery. Nat Rev Drug Discov. 2011;10(10):749–765.
  • Gleeson MP, Hersey A, Montanari D, et al. Probing the links between in vitro potency, admet and physicochemical parameters. Nat Rev Drug Discov. 2011;10(3):197–208.
  • Walters WP, Green J, Weiss JR, et al. What do medicinal chemists actually make? A 50-year retrospective. J Med Chem. 2011;54(19):6405–6416.
  • Leeson PD, Springthorpe B. The influence of drug-like concepts on decision-making in medicinal chemistry. Nat Rev Drug Discov. 2007;6(11):881–890.
  • Gleeson MP. Generation of a set of simple, interpretable admet rules of thumb. J Med Chem. 2008;51(4):817–834.
  • Waring MJ. Liphophilicity in drug discovery. Expert Opin Drug Discov. 2010;5(3):235–238.
  • Hann MM, Keseru GM. Finding the sweet spot: the role of nature and nurture in medicinal chemistry. Nat Rev Drug Discov. 2012;11(5):355–365.
  • Waring MJ, Arrowsmith J, Leach AR, et al. An analysis of the attrition of drug candidates from four major pharmaceutical companies. Nat Rev Drug Discov. 2015;14(7):475–486.
  • Meanwell NA. Improving drug candidates by design: A focus on physicochemical properties as a means of improving compound disposition and safety. Chem Res Toxicol. 2011;24(9):1420–1456.
  • Keseru GM, Makara GM. The influence of lead discovery strategies on the properties of drug candidates. Nat Rev Drug Discov. 2009;8(3):203–212.
  • Tarcsay A, Nyiri K, Keseru GM. Impact of lipophilic efficiency on compound quality. J Med Chem. 2012;55(3):1252–1260.
  • Leeson PD. Molecular inflation, attrition and the rule of five. Adv Drug Deliv Rev. 2016;101:22–33.
  • Leeson PD, Young RJ. Molecular property design: does everyone get it? ACS Med Chem Lett. 2015;6(7):722–725.

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