Betulinic acid and its derivatives as anti-angiogenic agents

被引：68
作者：
Mukherjee, R
Jaggi, M
Rajendran, P
Siddiqui, MJA
Srivastava, SK
Vardhan, A
Burman, AC
机构：
[1] Dabur Res Fdn, Div Expt Oncol, Ghaziabad 201010, Uttar Pradesh, India
[2] Dabur Res Fdn, Chem Res, Ghaziabad 201010, Uttar Pradesh, India
[3] Dabur Res Fdn, Med Chem, Ghaziabad 201010, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 09期
关键词：
D O I：
10.1016/j.bmcl.2004.02.044
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Betulinic acid (1) significantly caused cytotoxicity to endothelial cell line ECV304 (IC50 1.26 +/- 0.44 mug/mL) in a 5-day MTT assay. Novel and more potent derivatives of betulinic acid (2, 4, 6-8) have been synthesized with IC50 less than 0.4 mug/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further betulinic acid (1) inhibited TLS formation of ECV304 cells on Matrigel(TM) by 5.5% while its derivatives caused an inhibition of 13.1-49.2%. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2181 / 2184
页数：4
相关论文
共 12 条
  • [1] ANDERSON BM, Patent No. 9504526
  • [2] CONTROLLED DELIVERY OF TAXOL FROM MICROSPHERES COMPOSED OF A BLEND OF ETHYLENE-VINYL ACETATE COPOLYMER AND POLY (D,L-LACTIC ACID)
    BURT, HM
    JACKSON, JK
    BAINS, SK
    LIGGINS, RT
    OKTABA, AMC
    ARSENAULT, AL
    HUNTER, WL
    [J]. CANCER LETTERS, 1995, 88 (01) : 73 - 79
  • [3] Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection
    Cichewicz, RH
    Kouzi, SA
    [J]. MEDICINAL RESEARCH REVIEWS, 2004, 24 (01) : 90 - 114
  • [4] TAXOL ENCAPSULATION IN POLY(EPSILON-CAPROLACTONE) MICROSPHERES
    DORDUNOO, SK
    JACKSON, JK
    ARSENAULT, LA
    OKTABA, AMC
    HUNTER, WL
    BURT, HM
    [J]. CANCER CHEMOTHERAPY AND PHARMACOLOGY, 1995, 36 (04) : 279 - 282
  • [5] Folkman Judah, 1997, P3075
  • [6] Jaggi M., 2001, US Patent, Patent No. [6228850 B1, 6228850]
  • [7] RAPID COLORIMETRIC ASSAY FOR CELLULAR GROWTH AND SURVIVAL - APPLICATION TO PROLIFERATION AND CYTO-TOXICITY ASSAYS
    MOSMANN, T
    [J]. JOURNAL OF IMMUNOLOGICAL METHODS, 1983, 65 (1-2) : 55 - 63
  • [8] DISCOVERY OF BETULINIC ACID AS A SELECTIVE INHIBITOR OF HUMAN-MELANOMA THAT FUNCTIONS BY INDUCTION OF APOPTOSIS
    PISHA, E
    CHAI, H
    LEE, IS
    CHAGWEDERA, TE
    FARNSWORTH, NR
    CORDELL, GA
    BEECHER, CWW
    FONG, HHS
    KINGHORN, AD
    BROWN, DM
    WANI, MC
    WALL, ME
    HIEKEN, TJ
    DASGUPTA, TK
    PEZZUTO, JM
    [J]. NATURE MEDICINE, 1995, 1 (10) : 1046 - 1051
  • [9] Ramadoss S., 2000, Use of betulinic acid and its derivatives for inhibiting cancer growth and a method of monitoring this, Patent No. [US6048847, 6048847]
  • [10] Ramadoss S., 1998, Pat, Patent No. [6,214,814 US, 6214814]
12