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Literature DB >> 11814794

Design, synthesis and biological activity of novel C2-C3' N-Linked macrocyclic taxoids.

Iwao Ojima¹, Xudong Geng, Songnian Lin, Paula Pera, Ralph J Bernacki.

Abstract

A series of novel macrocyclic taxoids was designed and synthesized by connecting the C-2 and C-3' N positions of the taxoid framework with various tethers. Cytotoxicity of these macrocyclic taxoids was evaluated against a human breast cancer cell line LCC6-WT, and a couple of the taxoids exhibited 0.09-0.3 microM IC(50) values.

Entities: Chemical Disease Gene Species

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Year: 2002 PMID： 11814794 DOI： 10.1016/s0960-894x(01)00747-8

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

6 in total

1. Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.

Authors: Thota Ganesh; Chao Yang; Andrew Norris; Tom Glass; Susan Bane; Rudravajhala Ravindra; Abhijit Banerjee; Belhu Metaferia; Shala L Thomas; Paraskevi Giannakakou; Ana A Alcaraz; Ami S Lakdawala; James P Snyder; David G I Kingston
Journal: J Med Chem Date: 2007-01-31 Impact factor: 7.446

2. Rotational-echo double-resonance NMR distance measurements for the tubulin-bound Paclitaxel conformation.

Authors: Younkee Paik; Chao Yang; Belhu Metaferia; Shoubin Tang; Susan Bane; Rudravajhala Ravindra; Natasha Shanker; Ana A Alcaraz; Scott A Johnson; Jacob Schaefer; Robert D O'Connor; Lynette Cegelski; James P Snyder; David G I Kingston
Journal: J Am Chem Soc Date: 2007-01-17 Impact factor: 15.419

3. Bridging converts a noncytotoxic nor-paclitaxel derivative to a cytotoxic analogue by constraining it to the T-Taxol conformation.

Authors: Shoubin Tang; Chao Yang; Peggy Brodie; Susan Bane; Rudravajhala Ravindra; Shubhada Sharma; Yi Jiang; James P Snyder; David G I Kingston
Journal: Org Lett Date: 2006-08-31 Impact factor: 6.005

Design, synthesis and biological activity of novel C2-C3' N-Linked macrocyclic taxoids.

1. Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.

2. Rotational-echo double-resonance NMR distance measurements for the tubulin-bound Paclitaxel conformation.

3. Bridging converts a noncytotoxic nor-paclitaxel derivative to a cytotoxic analogue by constraining it to the T-Taxol conformation.

4. Design, synthesis, and biological evaluation of novel C14-C3'BzN-linked macrocyclic taxoids.

Review 5. Recent advances in the study of the bioactive conformation of taxol.

6. A natural love of natural products.