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Page 1
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Taveras AG, Deskus J, Chao J, Vaccaro CJ, Njoroge FG, Vibulbhan B, Pinto P, Remiszewski S, del Rosario J, Doll RJ, Alvarez C, Lalwani T, Mallams AK, Rossman RR, Afonso A, Girijavallabhan VM, Ganguly AK, Pramanik B, Heimark L, Bishop WR, Wang L, Kirschmeier P, James L, Carr D, Liu M, et al. Taveras AG, et al. Among authors: mallams ak. J Med Chem. 1999 Jul 15;42(14):2651-61. doi: 10.1021/jm990059k. J Med Chem. 1999. PMID: 10411485
Antitumor 8-chlorobenzocycloheptapyridines: a new class of selective, nonpeptidic, nonsulfhydryl inhibitors of ras farnesylation.
Mallams AK, Njoroge FG, Doll RJ, Snow ME, Kaminski JJ, Rossman RR, Vibulbhan B, Bishop WR, Kirschmeier P, Liu M, Bryant MS, Alvarez C, Carr D, James L, King I, Li Z, Lin CC, Nardo C, Petrin J, Remiszewski SW, Taveras AG, Wang S, Wong J, Catino J, Ganguly AK, et al. Mallams AK, et al. Bioorg Med Chem. 1997 Jan;5(1):93-9. doi: 10.1016/s0968-0896(96)00205-2. Bioorg Med Chem. 1997. PMID: 9043661
Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.
Mallams AK, Rossman RR, Doll RJ, Girijavallabhan VM, Ganguly AK, Petrin J, Wang L, Patton R, Bishop WR, Carr DM, Kirschmeier P, Catino JJ, Bryant MS, Chen KJ, Korfmacher WA, Nardo C, Wang S, Nomeir AA, Lin CC, Li Z, Chen J, Lee S, Dell J, Lipari P, Liu M, et al. Mallams AK, et al. J Med Chem. 1998 Mar 12;41(6):877-93. doi: 10.1021/jm970462w. J Med Chem. 1998. PMID: 9526562
Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.
Liu M, Bryant MS, Chen J, Lee S, Yaremko B, Lipari P, Malkowski M, Ferrari E, Nielsen L, Prioli N, Dell J, Sinha D, Syed J, Korfmacher WA, Nomeir AA, Lin CC, Wang L, Taveras AG, Doll RJ, Njoroge FG, Mallams AK, Remiszewski S, Catino JJ, Girijavallabhan VM, Bishop WR, et al. Liu M, et al. Among authors: mallams ak. Cancer Res. 1998 Nov 1;58(21):4947-56. Cancer Res. 1998. PMID: 9810004
(+)-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.
Njoroge FG, Taveras AG, Kelly J, Remiszewski S, Mallams AK, Wolin R, Afonso A, Cooper AB, Rane DF, Liu YT, Wong J, Vibulbhan B, Pinto P, Deskus J, Alvarez CS, del Rosario J, Connolly M, Wang J, Desai J, Rossman RR, Bishop WR, Patton R, Wang L, Kirschmeier P, Ganguly AK, et al. Njoroge FG, et al. Among authors: mallams ak. J Med Chem. 1998 Nov 19;41(24):4890-902. doi: 10.1021/jm980462b. J Med Chem. 1998. PMID: 9822558
Effects of SCH 59228, an orally bioavailable farnesyl protein transferase inhibitor, on the growth of oncogene-transformed fibroblasts and a human colon carcinoma xenograft in nude mice.
Liu M, Bryant MS, Chen J, Lee S, Yaremko B, Li Z, Dell J, Lipari P, Malkowski M, Prioli N, Rossman RR, Korfmacher WA, Nomeir AA, Lin CC, Mallams AK, Doll RJ, Catino JJ, Girijavallabhan VM, Kirschmeier P, Bishop WR. Liu M, et al. Among authors: mallams ak. Cancer Chemother Pharmacol. 1999;43(1):50-8. doi: 10.1007/s002800050862. Cancer Chemother Pharmacol. 1999. PMID: 9923541
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.
Strickland CL, Weber PC, Windsor WT, Wu Z, Le HV, Albanese MM, Alvarez CS, Cesarz D, del Rosario J, Deskus J, Mallams AK, Njoroge FG, Piwinski JJ, Remiszewski S, Rossman RR, Taveras AG, Vibulbhan B, Doll RJ, Girijavallabhan VM, Ganguly AK. Strickland CL, et al. Among authors: mallams ak. J Med Chem. 1999 Jun 17;42(12):2125-35. doi: 10.1021/jm990030g. J Med Chem. 1999. PMID: 10377218
SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53.
Demma M, Maxwell E, Ramos R, Liang L, Li C, Hesk D, Rossman R, Mallams A, Doll R, Liu M, Seidel-Dugan C, Bishop WR, Dasmahapatra B. Demma M, et al. J Biol Chem. 2010 Apr 2;285(14):10198-212. doi: 10.1074/jbc.M109.083469. Epub 2010 Feb 2. J Biol Chem. 2010. PMID: 20124408 Free PMC article.
30 results