Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

Hwan Mook Kim; Kiho Lee; Bum Woo Park; Dong Kyu Ryu; Kangjeon Kim; Chang Woo Lee; Song Kyu Park; Jung Whan Han; Hee Yoon Lee; Hyun Yong Lee; Gyoonhee Han

doi:10.1016/j.bmcl.2006.04.091

Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

Hwan Mook Kim, Kiho Lee, Bum Woo Park, Dong Kyu Ryu, Kangjeon Kim, Chang Woo Lee, Song Kyu Park, Jung Whan Han, Hee Yoon Lee, Hyun Yong Lee, Gyoonhee Han

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

30 Citations (Scopus)

Abstract

δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.

Original language	English
Pages (from-to)	4068-4070
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2006.04.091
Publication status	Published - 2006 Aug 1

Bibliographical note

Funding Information:
This research was supported by a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Wellfare, and the Ministry of Commerce, Industry and Energy, the Republic of Korea.

All Science Journal Classification (ASJC) codes

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

UN SDGs

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

Access to Document

10.1016/j.bmcl.2006.04.091

Cite this

Kim, H. M., Lee, K., Park, B. W., Ryu, D. K., Kim, K., Lee, C. W., Park, S. K., Han, J. W., Lee, H. Y., Lee, H. Y., & Han, G. (2006). Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(15), 4068-4070. https://doi.org/10.1016/j.bmcl.2006.04.091

@article{9c3460b32bf9498aba059d956c7b5407,

title = "Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors",

abstract = "δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.",

author = "Kim, {Hwan Mook} and Kiho Lee and Park, {Bum Woo} and Ryu, {Dong Kyu} and Kangjeon Kim and Lee, {Chang Woo} and Park, {Song Kyu} and Han, {Jung Whan} and Lee, {Hee Yoon} and Lee, {Hyun Yong} and Gyoonhee Han",

note = "Funding Information: This research was supported by a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Wellfare, and the Ministry of Commerce, Industry and Energy, the Republic of Korea.",

year = "2006",

month = aug,

day = "1",

doi = "10.1016/j.bmcl.2006.04.091",

language = "English",

volume = "16",

pages = "4068--4070",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "15",

}

TY - JOUR

T1 - Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

AU - Kim, Hwan Mook

AU - Lee, Kiho

AU - Park, Bum Woo

AU - Ryu, Dong Kyu

AU - Kim, Kangjeon

AU - Lee, Chang Woo

AU - Park, Song Kyu

AU - Han, Jung Whan

AU - Lee, Hee Yoon

AU - Lee, Hyun Yong

AU - Han, Gyoonhee

N1 - Funding Information: This research was supported by a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Wellfare, and the Ministry of Commerce, Industry and Energy, the Republic of Korea.

PY - 2006/8/1

Y1 - 2006/8/1

N2 - δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.

AB - δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.

UR - http://www.scopus.com/inward/record.url?scp=33745140574&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33745140574&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.04.091

DO - 10.1016/j.bmcl.2006.04.091

M3 - Article

C2 - 16723227

AN - SCOPUS:33745140574

SN - 0960-894X

VL - 16

SP - 4068

EP - 4070

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

Abstract

Bibliographical note

All Science Journal Classification (ASJC) codes

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this