Hybrid antitumor compounds containing a cyclic enediyne and a DN

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514422, 514383, 514397, 514407, 514343, 514340, 514341, 514290, 514314, 5482654, 5483111, 5483124, 5483137, 5483147, 5483641, 5483651, 548492, 548524, 546276, 546278, 546279, 546281, 546101, 546169, 546175, A61k 3140, A61k 3144, C07D20910, C07D20750, C07D40108, C07D23358

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053958497

ABSTRACT:
The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general formula (I)

REFERENCES:
D. L. Boger and J. Zhou, "CDPI.sub.3 -Enediyne and CDP1.sub.3 -EDTA Conjugates: A New Class of DNA Cleaving Agents", Journal of Organic Chemistry, 58, pp. 3018-3024, 1993.
K. C. Nicolaou, et al, "Chemistry and Biology of Natural and Designed Enediynes", Proceedings of the National Academy of Sciences, USA, 90, pp. 5881-5888, 1993.
K. C. Nicolaou and W. M. Dai, "Chemistry and Biology of the Enediyne Anticancer Antibiotics", Angewandte Chemie, 30, No. 11, pp. 1387-1416, 1991.
Masahiko Tokuda, et al, "Synthesis of a Hybrid Molecule Containing Neocarzinostatin Chromophore Analogue and Minor Groove Binder", Tetrahedron Letters, 34, No. 4, pp. 669-672, 1993.
K. Toshima, et al, "Design, Synthesis and DNA Cleaving Profiles of Hybrids Containing the Novel Enediyne and Naturally Occurring DNA Intercalators", Journal of the Chemical Society, Chemical Communications, USA, pp. 1525-1527, 1993.

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