Literature DB >> 2920809

Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4.

G R Pettit1, S B Singh, E Hamel, C M Lin, D S Alberts, D Garcia-Kendall.   

Abstract

The African tree Combretum caffrum (Combretacae) has been found to contain a powerful inhibitor of tubulin polymerization (IC50 2-3 microM), the growth of murine lymphocytic leukemia (L 1210 and P 388 with ED50 approximately 0.003 microM and human colon cancer cell lines [(e.g. LoVo (ED50 = 0.005 microgram/ml), HT 29 (ED50 0.02 microgram/ml, Colo 205 (ED50 = 0.07 microgram/ml), DLD-1 (ED50 = 0.005 microgram/ml) and HCT-15 (ED50 = 0.0009 microgram/ml] designated combretastatin A-4 (1c). The structure assigned by spectral techniques was confirmed by synthesis.

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Year:  1989        PMID： 2920809     DOI： 10.1007/BF01954881

Source DB:  PubMed          Journal:  Experientia        ISSN： 0014-4754


  1 in total

1.  Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum.

Authors:  G R Pettit; S B Singh; M L Niven; E Hamel; J M Schmidt
Journal:  J Nat Prod       Date:  1987 Jan-Feb       Impact factor: 4.050
  1 in total
  144 in total

1.  A pharmacokinetic and safety study of single dose intravenous combretastatin A4 phosphate in Chinese patients with refractory solid tumours.

Authors:  Xuexin He; Su Li; He Huang; Zhiming Li; Likun Chen; Sheng Ye; Jiajia Huang; Jing Zhan; Tongyu Lin
Journal:  Br J Clin Pharmacol       Date:  2011-06       Impact factor: 4.335

2.  Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.

Authors:  Romeo Romagnoli; Pier Giovanni Baraldi; Maria Kimatrai Salvador; Delia Preti; Mojgan Aghazadeh Tabrizi; Andrea Brancale; Xian-Hua Fu; Jun Li; Su-Zhan Zhang; Ernest Hamel; Roberta Bortolozzi; Giuseppe Basso; Giampietro Viola
Journal:  J Med Chem       Date:  2011-12-21       Impact factor: 7.446

3.  Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.

Authors:  Romeo Romagnoli; Pier Giovanni Baraldi; Olga Cruz-Lopez; Carlota Lopez Cara; Maria Dora Carrion; Andrea Brancale; Ernest Hamel; Longchuan Chen; Roberta Bortolozzi; Giuseppe Basso; Giampietro Viola
Journal:  J Med Chem       Date:  2010-05-27       Impact factor: 7.446

4.  Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model.

Authors:  Cheng-Huang Shen; Jia-Jen Shee; Jin-Yi Wu; Yi-Wen Lin; Jiann-Der Wu; Yi-Wen Liu
Journal:  Br J Pharmacol       Date:  2010-08       Impact factor: 8.739

5.  Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).

Authors:  Matthew T Macdonough; Tracy E Strecker; Ernest Hamel; John J Hall; David J Chaplin; Mary Lynn Trawick; Kevin G Pinney
Journal:  Bioorg Med Chem       Date:  2013-07-23       Impact factor: 3.641

Review 6.  A review and update of the current status of the vasculature-disabling agent combretastatin-A4 phosphate (CA4P).

Authors:  Dietmar W Siemann; David J Chaplin; Patricia A Walicke
Journal:  Expert Opin Investig Drugs       Date:  2009-02       Impact factor: 6.206

7.  Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.

Authors:  Haichan Niu; Tracy E Strecker; Jeni L Gerberich; James W Campbell; Debabrata Saha; Deboprosad Mondal; Ernest Hamel; David J Chaplin; Ralph P Mason; Mary Lynn Trawick; Kevin G Pinney
Journal:  J Med Chem       Date:  2019-05-24       Impact factor: 7.446

Review 8.  Targeting microtubules by natural agents for cancer therapy.

Authors:  Eiman Mukhtar; Vaqar Mustafa Adhami; Hasan Mukhtar
Journal:  Mol Cancer Ther       Date:  2014-01-16       Impact factor: 6.261

9.  Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors.

Authors:  Sultan Nacak Baytas; Nazan Inceler; Akin Yilmaz; Abdurrahman Olgac; Sevda Menevse; Erden Banoglu; Ernest Hamel; Roberta Bortolozzi; Giampietro Viola
Journal:  Bioorg Med Chem       Date:  2014-04-20       Impact factor: 3.641

10.  Anti-tumor activity and mechanisms of a novel vascular disrupting agent, (Z)-3,4',5-trimethoxylstilbene-3'-O-phosphate disodium (M410).

Authors:  Yu-Chen Cai; Yong Zou; Yan-Li Ye; Hong-Yi Sun; Quan-Guan Su; Zhi-Xin Wang; Zhao-Lei Zeng; Li-Jian Xian
Journal:  Invest New Drugs       Date:  2009-12-11       Impact factor: 3.850
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