PROTEIN-KINASE-C INHIBITORY ACTIVITIES OF BALANOL ANALOGS BEARING CARBOXYLIC-ACID REPLACEMENTS

被引：28

作者：

HEERDING, JM ^{[1
]}

LAMPE, JW ^{[1
]}

DARGES, JW ^{[1
]}

STAMPER, ML ^{[1
]}

机构：

[1] SPHINX PHARMACEUT,DEPT BIOMOLEC RES,DURHAM,NC 27707

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 16期

关键词：

D O I：

10.1016/0960-894X(95)00303-B

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A variety of balanol analogs bearing carboxylic acid replacements (amides, sulfonamides and tetrazoles) were synthesized and evaluated for protein kinase C (PKC) inhibitory activity. In general, those compounds which bear an acidic proton (pKa less than or equal to 7.6) display potent PKC activity, and show selectivity for PKC over other kinases. Prodrugs are excellent tools for increasing cellular activity of some acid replacements.

引用

页码：1839 / 1842

页数：4

共 16 条

[1] ALEXANDER J, 1994, J PHARM SCI, V22, P3549
[2] THERAPEUTIC POTENTIAL OF PROTEIN-KINASE-C INHIBITORS
BRADSHAW, D
HILL, CH
NIXON, JS
WILKINSON, SE
[J]. AGENTS AND ACTIONS, 1993, 38 (1-2): : 135 - 147
[3] NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF A SERIES OF N-(BIPHENYLYLMETHYL)IMIDAZOLES AS POTENT, ORALLY ACTIVE ANTIHYPERTENSIVES
CARINI, DJ
DUNCIA, JV
ALDRICH, PE
CHIU, AT
JOHNSON, AL
PIERCE, ME
PRICE, WA
SANTELLA, JB
WELLS, GJ
WEXLER, RR
WONG, PC
YOO, SE
TIMMERMANS, PBMWM
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) : 2525 - 2547
[4] DEFAUW JM, 1994, 24TH NAT MED CHEM S
[5] 3 SYNTHETIC ROUTES TO A STERICALLY HINDERED TETRAZOLE - A NEW ONE-STEP MILD CONVERSION OF AN AMIDE INTO A TETRAZOLE
DUNCIA, JV
PIERCE, ME
SANTELLA, JB
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1991, 56 (07) : 2395 - 2400
[6] 2 PRACTICAL SYNTHESES OF STERICALLY CONGESTED BENZOPHENONES
HOLLINSHEAD, SP
NICHOLS, JB
WILSON, JW
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1994, 59 (22) : 6703 - 6709
[7] NATURALLY-OCCURRING PROTEIN-KINASE-C INHIBITORS .2. ISOLATION OF OLIGOMERIC STILBENES FROM CARAGANA-SINICA
KULANTHAIVEL, P
JANZEN, WP
BALLAS, LM
JIANG, JB
HU, CQ
DARGES, JW
SELDIN, JC
COFIELD, DJ
ADAMS, LM
[J]. PLANTA MEDICA, 1995, 61 (01) : 41 - 44
[8] BALANOL - A NOVEL AND POTENT INHIBITOR OF PROTEIN-KINASE-C FROM THE FUNGUS VERTICILLIUM-BALANOIDES
KULANTHAIVEL, P
HALLOCK, YF
BOROS, C
HAMILTON, SM
JANZEN, WP
BALLAS, LM
LOOMIS, CR
JIANG, JB
KATZ, B
STEINER, JR
CLARDY, J
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1993, 115 (14) : 6452 - 6453
[9] TOTAL SYNTHESIS OF (-)-BALANOL
LAMPE, JW
HUGHES, PF
BIGGERS, CK
SMITH, SH
HU, H
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1994, 59 (18) : 5147 - 5148
[10] RATIONAL DESIGN OF 4-[(METHYLSULFONYL)AMINO]BENZAMIDES AS CLASS-III ANTIARRHYTHMIC AGENTS
LUMMA, WC
WOHL, RA
DAVEY, DD
ARGENTIERI, TM
DEVITA, RJ
GOMEZ, RP
JAIN, VK
MARISCA, AJ
MORGAN, TK
REISER, HJ
SULLIVAN, ME
WIGGINS, J
WONG, SS
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (05) : 755 - 758

← 1 2 →