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6 results on '"Truax, Valarie M."'

1. Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings

Author

Nguyen, Huy H., primary, Tahirovic, Yesim A., additional, Truax, Valarie M., additional, Wilson, Robert J., additional, Jecs, Edgars, additional, Miller, Eric J., additional, Kim, Michelle B., additional, Akins, Nicholas S., additional, Xu, Lingjie, additional, Jiang, Yi, additional, Wang, Tao, additional, Sum, Chi S., additional, Cvijic, Mary E., additional, Schroeder, Gretchen M., additional, Wilson, Lawrence J., additional, and Liotta, Dennis C., additional

Published
2021
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2. Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties

Author

Tahirovic, Yesim A., primary, Truax, Valarie M., additional, Wilson, Robert J., additional, Jecs, Edgars, additional, Nguyen, Huy H., additional, Miller, Eric J., additional, Kim, Michelle B., additional, Kuo, Katie M., additional, Wang, Tao, additional, Sum, Chi S., additional, Cvijic, Mary E., additional, Schroeder, Gretchen M., additional, Wilson, Lawrence J., additional, and Liotta, Dennis C., additional

Published
2018
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3. Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains

Author

Jecs, Edgars, primary, Miller, Eric J., additional, Wilson, Robert J., additional, Nguyen, Huy H., additional, Tahirovic, Yesim A., additional, Katzman, Brook M., additional, Truax, Valarie M., additional, Kim, Michelle B., additional, Kuo, Katie M., additional, Wang, Tao, additional, Sum, Chi S., additional, Cvijic, Mary E., additional, Schroeder, Gretchen M., additional, Wilson, Lawrence J., additional, and Liotta, Dennis C., additional

Published
2018
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4. Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists

Author

Wilson, Robert J., primary, Jecs, Edgars, additional, Miller, Eric J., additional, Nguyen, Huy H., additional, Tahirovic, Yesim A., additional, Truax, Valarie M., additional, Kim, Michelle B., additional, Kuo, Katie M., additional, Wang, Tao, additional, Sum, Chi Shing, additional, Cvijic, Mary E., additional, Paiva, Anthony A., additional, Schroeder, Gretchen M., additional, Wilson, Lawrence J., additional, and Liotta, Dennis C., additional

Published
2017
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5. Discovery of Tetrahydroisoquinoline-Based CXCR4 Antagonists

Author

Truax, Valarie M., primary, Zhao, Huanyu, additional, Katzman, Brooke M., additional, Prosser, Anthony R., additional, Alcaraz, Ana A., additional, Saindane, Manohar T., additional, Howard, Randy B., additional, Culver, Deborah, additional, Arrendale, Richard F., additional, Gruddanti, Prahbakar R., additional, Evers, Taylor J., additional, Natchus, Michael G., additional, Snyder, James P., additional, Liotta, Dennis C., additional, and Wilson, Lawrence J., additional

Published
2013
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6. Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.

Author

Jecs E, Miller EJ, Wilson RJ, Nguyen HH, Tahirovic YA, Katzman BM, Truax VM, Kim MB, Kuo KM, Wang T, Sum CS, Cvijic ME, Schroeder GM, Wilson LJ, and Liotta DC

Abstract

A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXCR4 inhibitor (IC 50 = 33 nM in CXCL12-mediated Ca 2+ flux) with enhanced stability in liver microsomes and reduced inhibition of CYP450 (2D6). The improved CXCR4 antagonist 15a has potential therapeutic application as a single agent or combinatory anticancer therapy., Competing Interests: The authors declare the following competing financial interest(s): D.C.L. is the principle investigator on a research grant from Bristol-Myers Squibb Research and Development to Emory University. D.C.L., L.J.W., E.J.M., E.J., H.H.N., Y.A.T., R.J.W., V.T.T., and M.B.K. are co-inventors on Emory-owned Intellectual Property that includes CXCR4 antagonists.

Published
2017
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