SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF COMBRETASTATIN ANALOGS - NAPHTHYLCOMBRETASTATINS AND RELATED-COMPOUNDS

被引：21

作者：

MEDARDE, M ^{[1
]}

DECLAIRAC, RPL ^{[1
]}

RAMOS, AC ^{[1
]}

CABALLERO, E ^{[1
]}

LOPEZ, JL ^{[1
]}

GRAVALOS, DG ^{[1
]}

SANFELICIANO, A ^{[1
]}

机构：

[1] PHARMA MAR SA,E-28780 TRES CANTOS,SPAIN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 03期

关键词：

D O I：

10.1016/0960-894X(95)00008-H

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Through a versatile synthesis of combretastatins we have prepared and assayed for activity some new compounds of this kind of antitumoral agents. Ketoderivatives (combretastatones) and other diphenylethane derivatives display low activity, but naphthylcombretastatin 3e shows activity comparable to that of the most potent combretastatins-B (dihydrocombretastatins), in spite of the lack of the 3-hydroxy-4-methoxyphenyl substructure considered to be neccesary for high antineoplastic potency.

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页码：229 / 232

页数：4

相关论文

共 18 条

[1] COMBRETATROPONES - HYBRIDS OF COMBRETASTATIN AND COLCHICINE - SYNTHESIS AND BIOCHEMICAL EVALUATION [J].

ANDRES, CJ ;

BERNARDO, JE ;

YAN, Q ;

HASTIE, SB ;

MACDONALD, TL .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (04) :565-570

[2] SYNTHESIS AND EVALUATION OF STILBENE AND DIHYDROSTILBENE DERIVATIVES AS POTENTIAL ANTICANCER AGENTS THAT INHIBIT TUBULIN POLYMERIZATION [J].

CUSHMAN, M ;

NAGARATHNAM, D ;

GOPAL, D ;

CHAKRABORTI, AK ;

LIN, CM ;

HAMEL, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) :2579-2588

[3] SYNTHESIS AND EVALUATION OF A SERIES OF BENZYLANILINE HYDROCHLORIDES AS POTENTIAL CYTOTOXIC AND ANTIMITOTIC AGENTS ACTING BY INHIBITION OF TUBULIN POLYMERIZATION [J].

CUSHMAN, M ;

HE, HM ;

LIN, CM ;

HAMEL, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (19) :2817-2821

[4] SYNTHESIS AND EVALUATION OF ANALOGS OF (Z)-1-(4-METHOXYPHENYL)-2-(3,4,5-TRIMETHOXYPHENYL)ETHENE AS POTENTIAL CYTOTOXIC AND ANTIMITOTIC AGENTS [J].

CUSHMAN, M ;

NAGARATHNAM, D ;

GOPAL, D ;

HE, HM ;

LIN, CM ;

HAMEL, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (12) :2293-2306

[5] SYNTHESIS OF ALKOXY-SUBSTITUTED DIARYL COMPOUNDS AND CORRELATION OF RING SEPARATION WITH INHIBITION OF TUBULIN POLYMERIZATION - DIFFERENTIAL ENHANCEMENT OF INHIBITORY EFFECTS UNDER SUBOPTIMAL POLYMERIZATION REACTION CONDITIONS [J].

GETAHUN, Z ;

JURD, L ;

CHU, PS ;

LIN, CM ;

HAMEL, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (06) :1058-1067

[6]

LIN CM, 1988, MOL PHARMACOL, V34, P200

[7] ANTIMITOTIC NATURAL-PRODUCTS COMBRETASTATIN-A-4 AND COMBRETASTATIN-A-2 - STUDIES ON THE MECHANISM OF THEIR INHIBITION OF THE BINDING OF COLCHICINE TO TUBULIN [J].

LIN, CM ;

HO, HH ;

PETTIT, GR ;

HAMEL, E .

BIOCHEMISTRY, 1989, 28 (17) :6984-6991

[8]

MCGOWN AT, 1989, ANTI-CANCER DRUG DES, V3, P249

[9] A VERSATILE APPROACH TO THE SYNTHESIS OF COMBRETASTATINS [J].

MEDARDE, M ;

DECLAIRAC, RPL ;

LOPEZ, JL ;

SANFELICIANO, A .

JOURNAL OF NATURAL PRODUCTS, 1994, 57 (08) :1136-1144

[10] QUANTITATIVE STRUCTURE - ACTIVITY RELATIONSHIP ANALYSIS OF COMBRETASTATINS - A CLASS OF NOVEL ANTIMITOTIC AGENTS [J].

NANDY, P ;

BANERJEE, S ;

GAO, H ;

HUI, MBV ;

LIEN, EJ .

PHARMACEUTICAL RESEARCH, 1991, 8 (06) :776-781