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9 results on '"Sum, Chi S."'

2. Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles

Author

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

Published
2022
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3. 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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4. Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties

Author

Nguyen, Huy H., primary, Kim, Michelle B., additional, Wilson, Robert J., additional, Butch, Christopher J., additional, Kuo, Katie M., additional, Miller, Eric J., additional, Tahirovic, Yesim A., additional, Jecs, Edgars, additional, Truax, Valarie 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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5. 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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6. Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties

Author

Miller, Eric J., primary, Jecs, Edgars, additional, Truax, Valarie M., additional, Katzman, Brooke M., additional, Tahirovic, Yesim A., additional, Wilson, Robert J., additional, Kuo, Katie M., additional, Kim, Michelle B., additional, Nguyen, Huy H., additional, Saindane, Manohar T., additional, Zhao, Huanyu, 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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7. 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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8. Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties

Author

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

Abstract

CXCR4 is a seven-transmembrane receptor expressed by hematopoietic stem cells and progeny, as well as by ≥48 different cancers types. CXCL12, the only chemokine ligand of CXCR4, is secreted within the tumor microenvironment, providing sanctuary for CXCR4+tumor cells from immune surveillance and chemotherapeutic elimination by (1) stimulating prosurvival signaling and (2) recruiting CXCR4+immunosuppressive leukocytes. Additionally, distant CXCL12-rich niches attract and support CXCR4+metastatic growths. Accordingly, CXCR4 antagonists can potentially obstruct CXCR4-mediated prosurvival signaling, recondition the CXCR4+leukocyte infiltrate from immunosuppressive to immunoreactive, and inhibit CXCR4+cancer cell metastasis. Current small molecule CXCR4 antagonists suffer from poor oral bioavailability and off-target liabilities. Herein, we report a series of novel tetrahydroisoquinoline-containing CXCR4 antagonists designed to improve intestinal absorption and off-target profiles. Structure–activity relationships regarding CXCR4 potency, intestinal permeability, metabolic stability, and cytochrome P450 inhibition are presented.

Published
2024
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9. 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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