Successful Drug Discovery, Volume 2 by Janos Fischer, Wayne E. Childers PDF

By Janos Fischer, Wayne E. Childers

ISBN-10: 3527341153

ISBN-13: 9783527341153

Keeping the winning procedure present in the former quantity during this sequence, the inventors and first builders of substances that effectively made it to industry inform the tale of the drug's discovery and improvement and relate the usually twisted direction from the 1st candidate molecule to the ultimate advertised drug.
eleven chosen case stories describe lately brought medications that experience now not been formerly coated in textbooks or common references. those diversity throughout six assorted healing fields and supply a consultant cross-section of the present drug improvement efforts. sponsored via copious information and chemical info, the perception and event of the participants makes this some of the most valuable education manuals junior medicinal chemist can desire to discover and has gained the aid and endorsement of IUPAC.

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4 Synthetic Analogues of the Zinc-Binding Thiol Natural Products The significance of such differences in selectivity for either therapeutic benefit or undesirable side effects is unclear. In our group, we have prepared these three natural products by total synthesis and tested them in proliferation assays with the MCF7 breast cancer cell line. While romidepsin and largazole are similar in activity with IC50 values of 1 and 5 nM respectively, thailandepsin A is more potent at 60 pM. The reasons for thailandepsin’s higher potency in cells compared to the mechanism-based assays are unclear.

Journal of Clinical Oncology, 27, 5410–5417. , McCulloch, W. H. (2010) Final results from a multicenter, international, pivotal study of romidepsin in refractory cutaneous T-cell lymphoma. Journal of Clinical Oncology, 28, 4485–4491. J. H. (2011) Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma. Journal of Antibiotics, 64, 525–531. , Pulitzer, M. and Querfeld, C. (2012) Management of cutaneous T cell lymphoma: new and emerging targets and treatment options.

Meanwhile, the UK biotech company Karus Therapeutics has adapted the Ganesan synthesis for the preparation of romidepsin and spiruchostatin analogues but details of lead compounds or their pharmacokinetics have not been disclosed [50, 51]. 5 Summary Romidepsin is the most famous example of the intriguing family of zinc-binding thiol natural products that are potent inhibitors of Class I HDACs. The compound has completed a 15-year odyssey from discovery by ‘big pharma’ to out-licensing to biotech and government-sponsored clinical trials before coming full circle and being acquired by big pharma after regulatory approval.

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Successful Drug Discovery, Volume 2 by Janos Fischer, Wayne E. Childers


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