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Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
Bioorg Med Chem Lett. 2004 Jul 16; 14(14):3659-63.BM

Abstract

Indenoisoquinolines and dihydroindenoisoquinolines have been synthesized possessing a nitro-substituted isoquinoline ring in an effort to explore the effects of electron-withdrawing substituents on biological activity. The in vitro anticancer activities of these molecules have been tested in the National Cancer Institute's screen of 55 cell lines. The compounds have also been tested for topoisomerase I (top1) inhibition. The results indicate that these substances are a potent class of top1 inhibitors with sub-micromolar cytotoxicity mean graph midpoints (MGM) and top1 inhibition equal to camptothecin.

Authors+Show Affiliations

Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

15203138

Citation

Morrell, Andrew, et al. "Synthesis of Nitrated Indenoisoquinolines as Topoisomerase I Inhibitors." Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 14, 2004, pp. 3659-63.
Morrell A, Antony S, Kohlhagen G, et al. Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors. Bioorg Med Chem Lett. 2004;14(14):3659-63.
Morrell, A., Antony, S., Kohlhagen, G., Pommier, Y., & Cushman, M. (2004). Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors. Bioorganic & Medicinal Chemistry Letters, 14(14), 3659-63.
Morrell A, et al. Synthesis of Nitrated Indenoisoquinolines as Topoisomerase I Inhibitors. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3659-63. PubMed PMID: 15203138.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors. AU - Morrell,Andrew, AU - Antony,Smitha, AU - Kohlhagen,Glenda, AU - Pommier,Yves, AU - Cushman,Mark, PY - 2004/03/30/received PY - 2004/05/12/revised PY - 2004/05/12/accepted PY - 2004/6/19/pubmed PY - 2005/2/8/medline PY - 2004/6/19/entrez SP - 3659 EP - 63 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 14 IS - 14 N2 - Indenoisoquinolines and dihydroindenoisoquinolines have been synthesized possessing a nitro-substituted isoquinoline ring in an effort to explore the effects of electron-withdrawing substituents on biological activity. The in vitro anticancer activities of these molecules have been tested in the National Cancer Institute's screen of 55 cell lines. The compounds have also been tested for topoisomerase I (top1) inhibition. The results indicate that these substances are a potent class of top1 inhibitors with sub-micromolar cytotoxicity mean graph midpoints (MGM) and top1 inhibition equal to camptothecin. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/15203138/Synthesis_of_nitrated_indenoisoquinolines_as_topoisomerase_I_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960894X04006572 DB - PRIME DP - Unbound Medicine ER -