Literature DB >> 15214797

Total synthesis and anti-tubulin activity of epi-c3 analogues of cryptophycin-24.

Suzanne B Buck1, Jacquelyn K Huff, Richard H Himes, Gunda I Georg.   

Abstract

Epi-C3-cryptophycin-24, epi-C3-m-chlorobenzyl-cryptophycin-24, and the corresponding styrenes were synthesized and tested in vitro against the MCF-7 and multidrug-resistant MCF-7/ADR breast cancer cell lines and in an in vitro tubulin assembly assay. The results demonstrate that the S configuration at the C3 stereocenter is not required to induce potent cytotoxicity and the m-Cl substituent present on the C10 side chain did not induce any large change in activity.

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Year:  2004        PMID: 15214797     DOI: 10.1021/jm030555f

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors.

Authors:  Cyril Barinka; Zora Novakova; Niyada Hin; Daniel Bím; Dana V Ferraris; Bridget Duvall; Gabriel Kabarriti; Reiji Tsukamoto; Milos Budesinsky; Lucia Motlova; Camilo Rojas; Barbara S Slusher; Tibor András Rokob; Lubomír Rulíšek; Takashi Tsukamoto
Journal:  Bioorg Med Chem       Date:  2018-11-14       Impact factor: 3.461

2.  Novel unit B cryptophycin analogues as payloads for targeted therapy.

Authors:  Eduard Figueras; Adina Borbély; Mohamed Ismail; Marcel Frese; Norbert Sewald
Journal:  Beilstein J Org Chem       Date:  2018-06-01       Impact factor: 2.883

Review 3.  Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy.

Authors:  Hao Chen; Zongtao Lin; Kinsie E Arnst; Duane D Miller; Wei Li
Journal:  Molecules       Date:  2017-08-01       Impact factor: 4.411

  3 in total

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