Benzenesulfonamides: A Unique Class of Chemokine Receptor Type 4 Inhibitors | Zendy

Mooring Suazette Reid | Zendy; Liu Jin | Zendy; Liang Zhongxing | Zendy; Ahn Jeffrey | Zendy; Hong Samuel | Zendy; Yoon Younghyoun | Zendy; Snyder James P. | Zendy; Shim Hyunsuk | Zendy

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Benzenesulfonamides: A Unique Class of Chemokine Receptor Type 4 Inhibitors

Author(s) -

Mooring Suazette Reid,

Liu Jin,

Liang Zhongxing,

Ahn Jeffrey,

Hong Samuel,

Yoon Younghyoun,

Snyder James P.,

Shim Hyunsuk

Publication year - 2013

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.201200582

Subject(s) - matrigel , cxcr4 , potency , in vitro , chemokine receptor , chemistry , ligand binding assay , receptor , cancer research , chemokine , biochemistry , biology , pharmacology

The interaction of CXCR4 with CXCL12 (SDF‐1) plays a critical role in cancer metastasis by facilitating the homing of tumor cells to metastatic sites. Based on our previously published work on CXCR4 antagonists, we have synthesized a series of aryl sulfonamides that inhibit the CXCR4/CXCL12 interaction. Analogue bioactivities were assessed with binding affinity and Matrigel invasion assays. Computer modeling was employed to evaluate a selection of the new analogues docked into the CXCR4 X‐ray structure and to rationalize discrepancies between the affinity and Matrigel in vitro assays. A lead compound displays nanomolar potency in the binding affinity assay (IC 50 =8.0 n M ) and the Matrigel invasion assay (100 % blockade of invasion at 10 n M ). These data demonstrate that benzenesulfonamides are a unique class of CXCR4 inhibitors with high potency.

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