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New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

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New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents. / Thanh Tung, Truong; Oanh, Dao Thi Kim; Dung, Phan Thi Phuong; Hue, Van Thi My; Park, Sang Ho; Han, Byung Woo; Kim, Youngsoo; Hong, Jin-Tae; Han, Sang-Bae; Nam, Nguyen-Hai.

I: Medicinal Chemistry, Bind 9, Nr. 8, 12.2013, s. 1051-7.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Harvard

Thanh Tung, T, Oanh, DTK, Dung, PTP, Hue, VTM, Park, SH, Han, BW, Kim, Y, Hong, J-T, Han, S-B & Nam, N-H 2013, 'New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents', Medicinal Chemistry, bind 9, nr. 8, s. 1051-7.

APA

Thanh Tung, T., Oanh, D. T. K., Dung, P. T. P., Hue, V. T. M., Park, S. H., Han, B. W., ... Nam, N-H. (2013). New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents. Medicinal Chemistry, 9(8), 1051-7.

Vancouver

Thanh Tung T, Oanh DTK, Dung PTP, Hue VTM, Park SH, Han BW o.a. New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents. Medicinal Chemistry. 2013 dec;9(8):1051-7.

Author

Thanh Tung, Truong ; Oanh, Dao Thi Kim ; Dung, Phan Thi Phuong ; Hue, Van Thi My ; Park, Sang Ho ; Han, Byung Woo ; Kim, Youngsoo ; Hong, Jin-Tae ; Han, Sang-Bae ; Nam, Nguyen-Hai. / New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents. I: Medicinal Chemistry. 2013 ; Bind 9, Nr. 8. s. 1051-7.

Bibtex

@article{a31810abcb0a4802860855ec1f2fdb1f,
title = "New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents",
abstract = "Results from clinical studies have demonstrated that inhibitors of histone deacetylase (HDAC) enzymes possess promise for the treatment of several types of cancer. Zolinza({\circledR}) (widely known as SAHA) has been approved by the FDA for the treatment of T-cell lymphoma. As a continuity of our ongoing research to find novel small molecules to target these important enzymes, we synthesized a series of benzothiazole-containing analogues of SAHA and found several compounds with very potent anticancer cytotoxicity. In this study, three more compounds of this type, including N(1)-(6-chlorobenzo[d]thiazol-2-yl)-N(8)-hydroxyoctanediamide (3a), N(1)-[6-(trifluoromethyl)benzo[d]thiazol-2-yl]-N(8)-hydroxyoctanediamide (3b) and N(1)-(thiazol-2-yl)-N(8)-hydroxyoctanediamide (6) were synthesized and evaluated for HDAC inhibition and cytotoxic activities. All three compounds showed very potent HDAC inhibitory effects. Docking revealed that both two compounds 3a, 3b showed higher affinities towards HDAC(8) compared to SAHA. In vitro, compound 3a exhibited cytotoxicity equipotent to SAHA against five human cancer cell lines. In term of in vivo activity, compound 3a demonstrated equivalent efficacy to SAHA in mouse xenograft model.",
author = "{Thanh Tung}, Truong and Oanh, {Dao Thi Kim} and Dung, {Phan Thi Phuong} and Hue, {Van Thi My} and Park, {Sang Ho} and Han, {Byung Woo} and Youngsoo Kim and Jin-Tae Hong and Sang-Bae Han and Nguyen-Hai Nam",
year = "2013",
month = "12",
language = "English",
volume = "9",
pages = "1051--7",
journal = "Medicinal Chemistry",
issn = "1573-4064",
publisher = "Bentham Science Publishers",
number = "8",

}

RIS

TY - JOUR

T1 - New benzothiazole/thiazole-containing hydroxamic acids as potent histone deacetylase inhibitors and antitumor agents

AU - Thanh Tung, Truong

AU - Oanh, Dao Thi Kim

AU - Dung, Phan Thi Phuong

AU - Hue, Van Thi My

AU - Park, Sang Ho

AU - Han, Byung Woo

AU - Kim, Youngsoo

AU - Hong, Jin-Tae

AU - Han, Sang-Bae

AU - Nam, Nguyen-Hai

PY - 2013/12

Y1 - 2013/12

N2 - Results from clinical studies have demonstrated that inhibitors of histone deacetylase (HDAC) enzymes possess promise for the treatment of several types of cancer. Zolinza(®) (widely known as SAHA) has been approved by the FDA for the treatment of T-cell lymphoma. As a continuity of our ongoing research to find novel small molecules to target these important enzymes, we synthesized a series of benzothiazole-containing analogues of SAHA and found several compounds with very potent anticancer cytotoxicity. In this study, three more compounds of this type, including N(1)-(6-chlorobenzo[d]thiazol-2-yl)-N(8)-hydroxyoctanediamide (3a), N(1)-[6-(trifluoromethyl)benzo[d]thiazol-2-yl]-N(8)-hydroxyoctanediamide (3b) and N(1)-(thiazol-2-yl)-N(8)-hydroxyoctanediamide (6) were synthesized and evaluated for HDAC inhibition and cytotoxic activities. All three compounds showed very potent HDAC inhibitory effects. Docking revealed that both two compounds 3a, 3b showed higher affinities towards HDAC(8) compared to SAHA. In vitro, compound 3a exhibited cytotoxicity equipotent to SAHA against five human cancer cell lines. In term of in vivo activity, compound 3a demonstrated equivalent efficacy to SAHA in mouse xenograft model.

AB - Results from clinical studies have demonstrated that inhibitors of histone deacetylase (HDAC) enzymes possess promise for the treatment of several types of cancer. Zolinza(®) (widely known as SAHA) has been approved by the FDA for the treatment of T-cell lymphoma. As a continuity of our ongoing research to find novel small molecules to target these important enzymes, we synthesized a series of benzothiazole-containing analogues of SAHA and found several compounds with very potent anticancer cytotoxicity. In this study, three more compounds of this type, including N(1)-(6-chlorobenzo[d]thiazol-2-yl)-N(8)-hydroxyoctanediamide (3a), N(1)-[6-(trifluoromethyl)benzo[d]thiazol-2-yl]-N(8)-hydroxyoctanediamide (3b) and N(1)-(thiazol-2-yl)-N(8)-hydroxyoctanediamide (6) were synthesized and evaluated for HDAC inhibition and cytotoxic activities. All three compounds showed very potent HDAC inhibitory effects. Docking revealed that both two compounds 3a, 3b showed higher affinities towards HDAC(8) compared to SAHA. In vitro, compound 3a exhibited cytotoxicity equipotent to SAHA against five human cancer cell lines. In term of in vivo activity, compound 3a demonstrated equivalent efficacy to SAHA in mouse xenograft model.

M3 - Journal article

C2 - 23521008

VL - 9

SP - 1051

EP - 1057

JO - Medicinal Chemistry

JF - Medicinal Chemistry

SN - 1573-4064

IS - 8

ER -

ID: 130698809