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

Genomic Medicine

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

12 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 (US)
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 - Feb 15 2014

Keywords

Degrasyn
Inhibitors
Jak2/Stat3
Multiple myeloma
Small molecules
Synthesis

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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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

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

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",

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

note = "Funding Information: The authors thank Cancer Center support Grant CA016672 for the support of the translational chemistry core Facility and NMR facility at M.D. Anderson Cancer Center. These studies were also partially supported by a grant from the Leukemia Lymphoma Society (to N.J.D.). ",

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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.

N1 - Funding Information: The authors thank Cancer Center support Grant CA016672 for the support of the translational chemistry core Facility and NMR facility at M.D. Anderson Cancer Center. These studies were also partially supported by a grant from the Leukemia Lymphoma Society (to N.J.D.).

PY - 2014/2/15

Y1 - 2014/2/15

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KW - Inhibitors

KW - Jak2/Stat3

KW - Multiple myeloma

KW - Small molecules

KW - Synthesis

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

Abstract

Keywords

ASJC Scopus subject areas

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