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

Zhenghong Peng; David S. Maxwell; Duoli Sun; Basvoju A. Bhanu Prasad; Paul T. Schuber; Ashutosh Pal; Yunming Ying; Dongmei Han; Liwei Gao; Shimei Wang; Alexander Levitzki; Vaibhav Kapuria; Moshe Talpaz; Matthew Young; Hollis D. Showalter; Nicholas J. Donato; William G. Bornmann

doi:10.1016/j.bmc.2013.12.048

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

Zhenghong Peng
, David S. Maxwell
, Duoli Sun
, Basvoju A. Bhanu Prasad
, Paul T. Schuber
, Ashutosh Pal
, Yunming Ying
, Dongmei Han
, Liwei Gao
, Shimei Wang
, Alexander Levitzki
, Vaibhav Kapuria
, Moshe Talpaz
, Matthew Young
, Hollis D. Showalter
, Nicholas J. Donato
, William G. Bornmann^*

^*Corresponding author for this work

Alexander Silberman Institute of Life Sciences

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

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.

Original language	English
Pages (from-to)	1450-1458
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	22
Issue number	4
DOIs	https://doi.org/10.1016/j.bmc.2013.12.048
State	Published - 15 Feb 2014

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Degrasyn
Inhibitors
Jak2/Stat3
Multiple myeloma
Small molecules
Synthesis

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10.1016/j.bmc.2013.12.048

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Peng, Z., Maxwell, D. S., Sun, D., Bhanu Prasad, B. A., Schuber, P. T., Pal, A., Ying, Y., Han, D., Gao, L., Wang, S., Levitzki, A., Kapuria, V., Talpaz, M., Young, M., Showalter, H. D., Donato, N. J., & Bornmann, W. G. (2014). Degrasyn-like symmetrical compounds: Possible therapeutic agents for multiple myeloma (MM-I). Bioorganic and Medicinal Chemistry, 22(4), 1450-1458. https://doi.org/10.1016/j.bmc.2013.12.048

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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.",

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doi = "10.1016/j.bmc.2013.12.048",

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Peng, Z, Maxwell, DS, Sun, D, Bhanu Prasad, BA, Schuber, PT, Pal, A, Ying, Y, Han, D, Gao, L, Wang, S, Levitzki, A, Kapuria, V, Talpaz, M, Young, M, Showalter, HD, Donato, NJ & Bornmann, WG 2014, 'Degrasyn-like symmetrical compounds: Possible therapeutic agents for multiple myeloma (MM-I)', Bioorganic and Medicinal Chemistry, vol. 22, no. 4, pp. 1450-1458. https://doi.org/10.1016/j.bmc.2013.12.048

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AU - Peng, Zhenghong

AU - Maxwell, David S.

AU - Sun, Duoli

AU - Bhanu Prasad, Basvoju A.

AU - Schuber, Paul T.

AU - Pal, Ashutosh

AU - Ying, Yunming

AU - Han, Dongmei

AU - Gao, Liwei

AU - Wang, Shimei

AU - Levitzki, Alexander

AU - Kapuria, Vaibhav

AU - Talpaz, Moshe

AU - Young, Matthew

AU - Showalter, Hollis D.

AU - Donato, Nicholas J.

AU - Bornmann, William G.

PY - 2014/2/15

Y1 - 2014/2/15

N2 - 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.

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KW - Degrasyn

KW - Inhibitors

KW - Jak2/Stat3

KW - Multiple myeloma

KW - Small molecules

KW - Synthesis

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JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 4

ER -

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

Abstract

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Keywords

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