• Publications
  • Influence
Complex formation between ethidium bromide and nucleic acids.
  • M. Waring
  • Chemistry, Medicine
  • Journal of molecular biology
  • 1 August 1965
TLDR
The interaction between ethidium bromide and nucleic acids shows a pronounced metachromatic effect which has been used to obtain quantitative data on the process of complex formation and is shown to be reversible in solution by demonstrating an exchange reaction between free and bound ethidium. Expand
An analysis of the attrition of drug candidates from four major pharmaceutical companies
TLDR
The compilation and analysis of combined data on the attrition of drug candidates from AstraZeneca, Eli Lilly and Company, GlaxoSmithKline and Pfizer reaffirms that control of physicochemical properties during compound optimization is beneficial in identifying compounds of candidate drug quality and indicates for the first time a link between the physic biochemical properties of compounds and clinical failure due to safety issues. Expand
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
TLDR
Following observations of significant tumor inhibition in preclinical models, the clinical candidate AZD9291 was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile. Expand
Assignment of DNA binding sites for 4',6-diamidine-2-phenylindole and bisbenzimide (Hoechst 33258). A comparative footprinting study.
TLDR
The DNA binding sites for DAPI and Hoechst 33258 are compared with those determined for the related minor groove-binding ligands, berenil, netropsin and distamycin A, under comparable conditions, and the importance of using different footprinting probes when analysing drug-DNA interactions is discussed. Expand
DNA sequence- and structure-selective alkylation of guanine N2 in the DNA minor groove by ecteinascidin 743, a potent antitumor compound from the Caribbean tunicate Ecteinascidia turbinata.
TLDR
Ecteinascidin 743 retarded the electrophoretic migration of both supercoiled and relaxed simian virus 40 DNA even in the presence of sodium dodecyl sulfate and after ethanol precipitation, consistent with covalent DNA modifications. Expand
Lipophilicity in drug discovery
  • M. Waring
  • Chemistry, Medicine
  • Expert opinion on drug discovery
  • 26 February 2010
TLDR
The aim is to provide an overview of the relevant literature in an attempt to summarise where the optimum region of lipophilicity lies and to highlight which particular issues and risks might be expected when operating outside this region. Expand
Molecular Aspects of Anticancer Drug/DNA Interactions
DNA topoisomerases, K. Kohn and R. Ralph the cellular and molecular pharmacology of the anthrapyrazole antitumour agent, D.R. Newell and L.H. Patterson calicheamicin, G.A. Elistad and W.D. DingExpand
Variation of the supercoils in closed circular DNA by binding of antibiotics and drugs: evidence for molecular models involving intercalation.
  • M. Waring
  • Chemistry, Medicine
  • Journal of molecular biology
  • 14 December 1970
TLDR
The effects of 17 substances on the S 20 of φX174 RF † DNA have been tested, investigating whether changes in the supercoiling of closed circles may be employed to verify intercalative binding and support for the intercalation model of Muller & Crothers (1968). Expand
DNA modification and cancer.
  • M. Waring
  • Biology, Medicine
  • Annual review of biochemistry
  • 1981
Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656
Glucokinase plays a central role in glucose homeostasis and small molecule activators of the glucokinase enzyme have been the subject of significant pharmaceutical research in the quest for agentsExpand
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