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

DOI: 10.1021/jm010531d

Source and publish data:

Journal of Medicinal Chemistry p. 2388 - 2409 (2002)

Update date:2022-07-31

Topics:

Authors:

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

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Article abstract of DOI:10.1021/jm010531d

A series of macrocyclic 3-aminopyrrolidinone farnesyltransferase inhibitors (FTIs) has been synthesized. Compared with previously described linear 3-aminopyrrolidinone FTIs such as compound 1, macrocycles such as 49 combined improved pharmacokinetic prope

Full text of DOI:10.1021/jm010531d

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