Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.

[1]  F. Caponigro,et al.  Farnesyl transferase inhibitors in clinical development , 2003, Expert opinion on investigational drugs.

[2]  C. Baum,et al.  Sch-66336 (sarasar) and other benzocycloheptapyridyl farnesyl protein transferase inhibitors: discovery, biology and clinical observations. , 2003, Current topics in medicinal chemistry.

[3]  N. Kemeny,et al.  A phase II trial of farnesyl protein transferase inhibitor SCH 66336, given by twice-daily oral administration, in patients with metastatic colorectal cancer refractory to 5-fluorouracil and irinotecan. , 2002, Annals of oncology : official journal of the European Society for Medical Oncology.

[4]  F. Lee,et al.  Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. , 2001, Cancer research.

[5]  F. G. N. A. V. M. Girijavallabhan.  Discovery and Advancement of Farnesyl Transferase Inhibitors as Potential Anticancer Therapeutic Agents: SCH 66336 a Case Study , 2001 .

[6]  W. R. Bishop,et al.  A Phase I trial of the farnesyl transferase inhibitor SCH66336: evidence for biological and clinical activity. , 2000, Cancer research.

[7]  P. Weber,et al.  Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. , 1999, Journal of medicinal chemistry.

[8]  Walter A. Korfmacher,et al.  Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. , 1998, Cancer research.

[9]  W. R. Bishop,et al.  (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. , 1998, Journal of medicinal chemistry.

[10]  W. R. Bishop,et al.  Novel Tricyclic Inhibitors of Farnesyl Protein Transferase , 1995, The Journal of Biological Chemistry.

[11]  A. Ganguly,et al.  Hydroxylated metabolites of loratadine: an example of conformational diastereomers due to atropisomerism , 1990 .

[12]  D. End.  Farnesyl Protein Transferase Inhibitors and Other Therapies Targeting the Ras Signal Transduction Pathway , 2004, Investigational New Drugs.

[13]  A. Adjei.  Protein farnesyl transferase as a target for the development of anticancer drugs , 2000 .

[14]  J. Sebolt-Leopold,et al.  RAS FARNESYLTRANSFERASE INHIBITORS , 1999 .