Literature DB >> 10498214

On topography and functionality in the B-D rings of cephalostatin cytotoxins.

T G LaCour1, C Guo, S Ma, J U Jeong, M R Boyd, S Matsunaga, N Fusetani, P L Fuchs.   

Abstract

Analogues 12'beta-hydroxycephalostatin 1 (9), 7'-deoxyritterazine G (10), and 14-epi-7'-deoxyritterazine B (11) were prepared via our protocol for unsymmetrical pyrazine synthesis. Cytotoxicity against human tumors was also determined for the first time for ritterazines, with femtomolar potency and a high correlation to cephalostatins observed. The SAR of these and related compounds provide insight into the importance of topography and certain chemical functionality in the B-D and B'-D' rings of cephalostatin type antineoplastics.

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Year:  1999        PMID: 10498214     DOI: 10.1016/s0960-894x(99)00430-8

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


  3 in total

Review 1.  Chemistry of trisdecacyclic pyrazine antineoplastics: the cephalostatins and ritterazines.

Authors:  Seongmin Lee; Thomas G LaCour; Philip L Fuchs
Journal:  Chem Rev       Date:  2009-06       Impact factor: 60.622

2.  Synthesis and evaluation of a fluorescent ritterazine-cephalostatin hybrid.

Authors:  Kanduluru Ananda Kumar; James J La Clair; Philip L Fuchs
Journal:  Org Lett       Date:  2011-09-14       Impact factor: 6.005

3.  Ritterostatin GN 1N , a Cephalostatin-Ritterazine Bis-steroidal Pyrazine Hybrid, Selectively Targets GRP78.

Authors:  Andrew J Ambrose; Evelyne A Santos; Paula C Jimenez; Danilo D Rocha; Diego V Wilke; Paolo Beuzer; Josh Axelrod; Ananda Kumar Kanduluru; Philip L Fuchs; Hu Cang; Letícia V Costa-Lotufo; Eli Chapman; James J La Clair
Journal:  Chembiochem       Date:  2017-02-02       Impact factor: 3.164

  3 in total

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