A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells

被引：91

作者：

Gediya, LK ^{[1
]}

Chopra, P ^{[1
]}

Purushottamachar, P ^{[1
]}

Maheshwari, N ^{[1
]}

Njar, VCO ^{[1
]}

机构：

[1] Univ Maryland, Sch Med, Dept Pharmacol & Expt Therapeut, Baltimore, MD 21201 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 15期

关键词：

D O I：

10.1021/jm058214k

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have developed a procedure for the synthesis of N-hydroxy-N-1-phenyloctanediamide (suberoylanilide hydroxamic acid (SAHA)), providing the product in 79.8% yield. SAHA is a potent inhibitor of histone deacetylase, induces differentiation and/or apoptosis in certain transformed cells in culture, and suppressed the growth of human prostate cancer LNCaP and PC-3 cell lines. The combination of SAHA with other compounds inhibited cell proliferation of LNCaP cells in additive fashion and resulted in synergistic growth inhibition.

引用

页码：5047 / 5051

页数：5

共 15 条

[1]

*AM CANC SOC WASH, 2005, CANC FACTS FIG

[2]

*AT PHARM INC, 2004, AT PHARM INC REC

[3]

Breslow R., 1993, PTC Int. Appl., Patent No. [WO93/07148, 9307148]

[4] A history of prostate cancer treatment [J].

Denmeade, SR ;

Isaacs, JT .

NATURE REVIEWS CANCER, 2002, 2 (05) :389-396

[5] The development of androgen-independent prostate cancer [J].

Feldman, BJ ;

Feldman, D .

NATURE REVIEWS CANCER, 2001, 1 (01) :34-45

[6] Cancer statistics, 2004 [J].

Jemal, A ;

Tiwari, RC ;

Murray, T ;

Ghafoor, A ;

Samuels, A ;

Ward, E ;

Feuer, EJ ;

Thun, MJ .

CA-A CANCER JOURNAL FOR CLINICIANS, 2004, 54 (01) :8-29

[7]

Kelly WK, 2003, CLIN CANCER RES, V9, P3578

[8] A new facile and expeditious synthesis of N-hydroxy-N′-phenyloctanediamide, a potent inducer of terminal cytodifferentiation [J].

Mai, A ;

Esposito, M ;

Sbardella, G ;

Massa, S .

ORGANIC PREPARATIONS AND PROCEDURES INTERNATIONAL, 2001, 33 (04) :391-394

[9] THE NUCLEAR RECEPTOR SUPERFAMILY - THE 2ND DECADE [J].

MANGELSDORF, DJ ;

THUMMEL, C ;

BEATO, M ;

HERRLICH, P ;

SCHUTZ, G ;

UMESONO, K ;

BLUMBERG, B ;

KASTNER, P ;

MARK, M ;

CHAMBON, P ;

EVANS, RM .

CELL, 1995, 83 (06) :835-839

[10] Nuclear receptor repression mediated by a complex containing SMRT, mSin3A, and histone deacetylase [J].

Nagy, L ;

Kao, HY ;

Chakravarti, D ;

Lin, RJ ;

Hassig, CA ;

Ayer, DE ;

Schreiber, SL ;

Evans, RM .

CELL, 1997, 89 (03) :373-380

← 1 2 →