2. Academic Validation
  3. Degrasyn-like symmetrical compounds: possible therapeutic agents for multiple myeloma (MM-I)

Degrasyn-like symmetrical compounds: possible therapeutic agents for multiple myeloma (MM-I)

  • Bioorg Med Chem. 2014 Feb 15;22(4):1450-8. doi: 10.1016/j.bmc.2013.12.048.
Zhenghong Peng 1,  David S Maxwell 1,  Duoli Sun 1,  Basvoju A Bhanu Prasad 1,  Paul T Schuber Jr 1,  Ashutosh Pal 2,  Yunming Ying 2,  Dongmei Han 2,  Liwei Gao 2,  Shimei Wang 2,  Alexander Levitzki 3,  Vaibhav Kapuria 4,  Moshe Talpaz 4,  Matthew Young 5,  Hollis D Showalter 6,  Nicholas J Donato 4,  William G Bornmann 7
Affiliations

Affiliations

  • 1 Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
  • 2 Department of Experimental Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
  • 3 Unit of Cellular Signaling, Department of Biological Chemistry, The Hebrew University of Jerusalem, Jerusalem, Israel.
  • 4 Department of Internal Medicine/Division of Hematology/Oncology, University of Michigan School of Medicine, Comprehensive Cancer Center, United States.
  • 5 Department of Pharmacology, University of Michigan School of Medicine, Comprehensive Cancer Center, United States.
  • 6 Department of Medicinal Chemistry, University of Michigan College of Pharmacy, Ann Arbor, MI 48109, United States.
  • 7 Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States. Electronic address: wbornmann@mdanderson.org.
PMID: 24457091 DOI: 10.1016/j.bmc.2013.12.048
Abstract

A series of degrasyn-like symmetrical compounds have been designed, synthesized, and screened against B cell malignancy (multiple myeloma, mantle cell lymphoma) cell lines. The lead compounds T5165804 and CP2005 showed higher nanomolar potency against these tumor cells in comparison to degrasyn and inhibited Usp9x activity in vitro and in intact cells. These observations suggest that this new class of compounds holds promise as Cancer therapeutic agents.

Keywords

Degrasyn; Inhibitors; Jak2/Stat3; Multiple myeloma; Small molecules; Synthesis.

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