A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo

被引：52

作者：

Jones, Philip ^{[1
]}

Altamura, Sergio ^{[1
]}

De Francesco, Raffaele ^{[1
]}

Paz, Odalys Gonzalez ^{[1
]}

Kinzel, Olaf ^{[1
]}

Mesiti, Giuseppe ^{[1
]}

Monteagudo, Edith ^{[1
]}

Pescatore, Giovanna ^{[1
]}

Rowley, Michael ^{[1
]}

Verdirame, Maria ^{[1
]}

Steinkijhler, Christian ^{[1
]}

机构：

[1] IRBM, Merck Res Labs, I-00040 Pomezia, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 08期

关键词：

D O I：

10.1021/jm800079s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin. These compounds show class I subtype selectivity and levels of cellular activity comparable to clinical candidates. A representative example has demonstrated tumor growth inhibition in a human colon HCT-116 carcinoma xenograft model comparable to known inhibitors.

引用

收藏

页码：2350 / 2353

页数：4

相关论文

共 29 条

[1] Anticancer activities of histone deacetylase inhibitors [J].

Bolden, Jessica E. ;

Peart, Melissa J. ;

Johnstone, Ricky W. .

NATURE REVIEWS DRUG DISCOVERY, 2006, 5 (09) :769-784

[2] Short-Chain Fatty Acid Inhibitors of Histone Deacetylases: Promising Anticancer Therapeutics? [J].

Chen, James S. ;

Faller, Douglas V. ;

Spanjaard, Remco A. .

CURRENT CANCER DRUG TARGETS, 2003, 3 (03) :219-236

[3] Acetylation and chromosomal functions [J].

Cheung, WL ;

Briggs, SD ;

Allis, CD .

CURRENT OPINION IN CELL BIOLOGY, 2000, 12 (03) :326-333

[4] Apicidin: A novel antiprotozoal agent that inhibits parasite histone deacetylase [J].

DarkinRattray, SJ ;

Gurnett, AM ;

Myers, RW ;

Dulski, PM ;

Crumley, TM ;

Allocco, JJ ;

Cannova, C ;

Meinke, PT ;

Colletti, SL ;

Bednarek, MA ;

Singh, SB ;

Goetz, MA ;

Dombrowski, AW ;

Polishook, JD ;

Schmatz, DM .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1996, 93 (23) :13143-13147

[5] Histone deacetylases (HDACs): characterization of the classical HDAC family [J].

De Ruijter, AJM ;

Van Gennip, AH ;

Caron, HN ;

Kemp, S ;

Van Kuilenburg, ABP .

BIOCHEMICAL JOURNAL, 2003, 370 :737-749

[6] Chromatin remodeling, cancer and chemotherapy [J].

Dey, Pranab .

CURRENT MEDICINAL CHEMISTRY, 2006, 13 (24) :2909-2919

[7] Trifluoromethyl ketones as inhibitors of histone deacetylase [J].

Frey, RR ;

Wada, CK ;

Garland, RB ;

Curtin, ML ;

Michaelides, MR ;

Li, JL ;

Pease, LJ ;

Glaser, KB ;

Marcotte, PA ;

Bouska, JJ ;

Murphy, SS ;

Davidsen, SK .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (23) :3443-3447

[8] Vorinostat [J].

Grant, Steven ;

Easley, Chris ;

Kirkpatrick, Peter .

NATURE REVIEWS DRUG DISCOVERY, 2007, 6 (01) :21-22

[9] From natural products to small molecule ketone histone deacetylase inhibitors:: Development of new class specific agents [J].

Jones, Philip ;

Steinkuhler, Christian .

CURRENT PHARMACEUTICAL DESIGN, 2008, 14 (06) :545-561

[10] A series of novel, potent, and selective histone deacetylase inhibitors [J].

Jones, Philip ;

Altamura, Sergio ;

Chakravarty, Prasun K. ;

Cecchetti, Ottavia ;

De Francesco, Raffaele ;

Gallinari, Paola ;

Ingenito, Raffaele ;

Meinke, Peter T. ;

Petrocchi, Alessia ;

Rowley, Michael ;

Scarpelli, Rita ;

Serafini, Sergio ;

Steinkuhler, Christian .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (23) :5948-5952