A fluorine scan of the phenylamidinium needle of tricyclic thrombin inhibitors: effects of fluorine substitution on p K a and binding affinity and evidence for …

J Olsen, P Seiler, B Wagner, H Fischer…

Index: Organic and Biomolecular Chemistry, , vol. 2, # 9 p. 1339 - 1352

Full Text: HTML

Citation Number: 65

Abstract

... The importance of organofluorine in medicinal chemistry has been increasing ever since the ... 2 In contrast, modulation of the physico-chemical properties (such as lipophilicity, metabolic ... it has become clear from crystallographic and computational studies that organic C–F is a ...

Related Articles:

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency

[Bell, Ian M.; Gallicchio, Steven N.; Abrams, Marc; Beese, Lorena S.; Beshore, Douglas C.; Bhimnathwala, Hema; Bogusky, Michael J.; Buser, Carolyn A.; Culberson, J. Christopher; Davide, Joseph; Ellis-Hutchings, Michelle; Fernandes, Christine; Gibbs, Jackson B.; Graham, Samuel L.; Hamilton, Kelly A.; Hartman, George D.; Heimbrook, David C.; Homnick, Carl F.; Huber, Hans E.; Huff, Joel R.; Kassahun, Kelem; Koblan, Kenneth S.; Kohl, Nancy E.; Lobell, Robert B.; Lynch Jr., Joseph J.; Robinson, Ronald; Rodrigues, A. David; Taylor, Jeffrey S.; Walsh, Eileen S.; Williams, Theresa M.; Zartmant, C. Blair Journal of Medicinal Chemistry, 2002 , vol. 45, # 12 p. 2388 - 2409]

A fluorine scan of the phenylamidinium needle of tricyclic thrombin inhibitors: effects of fluorine substitution on p K a and binding affinity and evidence for …

[Olsen, Jacob; Seiler, Paul; Wagner, Bjoern; Fischer, Holger; Tschopp, Thomas; Obst-Sander, Ulrike; Banner, David W.; Kansy, Manfred; Mueller, Klaus; Diederich, Francois Organic and Biomolecular Chemistry, 2004 , vol. 2, # 9 p. 1339 - 1352]

Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents

[Journal of Medicinal Chemistry, , vol. 46, # 14 p. 2973 - 2984]

Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents

[Journal of Medicinal Chemistry, , vol. 46, # 14 p. 2973 - 2984]

Asymmetric synthesis of α, α-diaryl and α-aryl-α-heteroaryl alkylamines by organometallic additions to N-tert-butanesulfinyl ketimines

[Tetrahedron Letters, , vol. 42, # 41 p. 7173 - 7176]

More Articles...