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Page 1
Dibasic benzo[b]thiophene derivatives as a novel class of active site-directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure-activity relationships, and binding orientation.
Sall DJ, Bastian JA, Briggs SL, Buben JA, Chirgadze NY, Clawson DK, Denney ML, Giera DD, Gifford-Moore DS, Harper RW, Hauser KL, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Palkowitz AD, Smith GF, Takeuchi K, Thrasher KJ, Tinsley JM, Utterback BG, Yan SC, Zhang M. Sall DJ, et al. Among authors: bastian ja. J Med Chem. 1997 Oct 24;40(22):3489-93. doi: 10.1021/jm9704107. J Med Chem. 1997. PMID: 9357512 No abstract available.
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.
Zhang M, Bailey DL, Bastian JA, Briggs SL, Chirgadze NY, Clawson DK, Denney ML, Gifford-Moore DS, Harper RW, Johnson LM, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Richett ME, Sall DJ, Smith AJ, Smith GF, Snyder DW, Takeuchi K, Utterback BG, Yan SC. Zhang M, et al. Among authors: bastian ja. Bioorg Med Chem Lett. 1999 Mar 8;9(5):775-80. doi: 10.1016/s0960-894x(99)00074-8. Bioorg Med Chem Lett. 1999. PMID: 10201846
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Potency, efficacy, and pharmacokinetic properties of modified C-3 side chain derivatives.
Sall DJ, Bailey DL, Bastian JA, Buben JA, Chirgadze NY, Clemens-Smith AC, Denney ML, Fisher MJ, Giera DD, Gifford-Moore DS, Harper RW, Johnson LM, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Palkowitz AD, Richett ME, Smith GF, Snyder DW, Takeuchi K, Toth JE, Zhang M. Sall DJ, et al. Among authors: bastian ja. J Med Chem. 2000 Feb 24;43(4):649-63. doi: 10.1021/jm9903388. J Med Chem. 2000. PMID: 10691691
D-phenylglycinol-derived non-covalent factor Xa inhibitors: effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity.
Klimkowski VJ, Watson BM, Wiley MR, Liebeschuetz J, Franciskovich JB, Marimuthu J, Bastian JA, Sall DJ, Smallwood JK, Chirgadze NY, Smith GF, Foster RS, Craft T, Sipes P, Chastain M, Sheehan SM. Klimkowski VJ, et al. Among authors: bastian ja. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5801-5. doi: 10.1016/j.bmcl.2007.08.051. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17881231
Imlunestrant is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wildtype and Mutant Breast Cancer.
Bhagwat SV, Mur C, Vandekopple M, Zhao B, Shen W, Marugán C, Capen A, Kindler L, Stephens JR, Huber L, Castanares MA, Garcia-Tapia D, Cohen JD, Bastian J, Mattioni B, Yuen E, Baker TK, Rodriguez Cruz V, Fei D, Manro JR, Pulliam N, Dowless MS, Ortiz Ruiz MJ, Yu C, Puca L, Klippel A, Bacchion F, Ismail-Khan R, Rodrik-Outmezguine V, Peng SB, Lallena MJ, Gong X, de Dios A. Bhagwat SV, et al. Cancer Res. 2024 Dec 9. doi: 10.1158/0008-5472.CAN-24-2608. Online ahead of print. Cancer Res. 2024. PMID: 39652577