Antineoplastic Agents. 592. Highly Effective Cancer Cell Growth Inhibitory Structural Modifications of Dolastatin 10
The dolastatin series of unique peptides, origi-nally discovered as constituents of the sea hare Dolabella auricularia, is of increasing importance in providing biological leads, especially to new and useful anticancer drugs. Dolastatin 10 and three analogues, minor structural modifications designat...
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| Veröffentlicht in: | Journal of natural products (Washington, D.C.) D.C.), 2011-05, Vol.74 (5), p.962-968 |
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| container_title | Journal of natural products (Washington, D.C.) |
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| creator | Pettit, George R Hogan, Fiona Toms, Steven |
| description | The dolastatin series of unique peptides, origi-nally discovered as constituents of the sea hare Dolabella auricularia, is of increasing importance in providing biological leads, especially to new and useful anticancer drugs. Dolastatin 10 and three analogues, minor structural modifications designated auristatins, are currently in human cancer clinical trials. The present study was undertaken to explore delivery to the cancer sites by way of phosphate or quinoline modifications. The initial objectives, auristatin TP as sodium phosphate 3b (GI50 10−2−10−4 μg/mL), auristatin 2-AQ (4, GI50 10−2−10−3 μg/mL), and auristatin 6-AQ (5, GI50 10−4 μg/mL), exhibited superior cancer cell growth inhibitory properties. |
| doi_str_mv | 10.1021/np1007334 |
| format | Article |
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The initial objectives, auristatin TP as sodium phosphate 3b (GI50 10−2−10−4 μg/mL), auristatin 2-AQ (4, GI50 10−2−10−3 μg/mL), and auristatin 6-AQ (5, GI50 10−4 μg/mL), exhibited superior cancer cell growth inhibitory properties.</description><identifier>ISSN: 0163-3864</identifier><identifier>ISSN: 1520-6025</identifier><identifier>EISSN: 1520-6025</identifier><identifier>DOI: 10.1021/np1007334</identifier><identifier>PMID: 21534541</identifier><identifier>CODEN: JNPRDF</identifier><language>eng</language><publisher>Northbrook, IL: American Chemical Society and American Society of Pharmacognosy</publisher><subject>Animals ; Antineoplastic agents ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Biological and medical sciences ; Clinical Trials as Topic ; Depsipeptides - chemistry ; Depsipeptides - pharmacology ; Drug Screening Assays, Antitumor ; General aspects ; Humans ; Leukemia P388 ; Medical sciences ; Mice ; Molecular Structure ; Pharmacology. 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The initial objectives, auristatin TP as sodium phosphate 3b (GI50 10−2−10−4 μg/mL), auristatin 2-AQ (4, GI50 10−2−10−3 μg/mL), and auristatin 6-AQ (5, GI50 10−4 μg/mL), exhibited superior cancer cell growth inhibitory properties.</description><subject>Animals</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Clinical Trials as Topic</subject><subject>Depsipeptides - chemistry</subject><subject>Depsipeptides - pharmacology</subject><subject>Drug Screening Assays, Antitumor</subject><subject>General aspects</subject><subject>Humans</subject><subject>Leukemia P388</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Molecular Structure</subject><subject>Pharmacology. 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Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Pettit, George R</creatorcontrib><creatorcontrib>Hogan, Fiona</creatorcontrib><creatorcontrib>Toms, Steven</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of natural products (Washington, D.C.)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pettit, George R</au><au>Hogan, Fiona</au><au>Toms, Steven</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antineoplastic Agents. 592. 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| identifier | ISSN: 0163-3864 |
| ispartof | Journal of natural products (Washington, D.C.), 2011-05, Vol.74 (5), p.962-968 |
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| source | MEDLINE; American Chemical Society Journals |
| subjects | Animals Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Clinical Trials as Topic Depsipeptides - chemistry Depsipeptides - pharmacology Drug Screening Assays, Antitumor General aspects Humans Leukemia P388 Medical sciences Mice Molecular Structure Pharmacology. Drug treatments |
| title | Antineoplastic Agents. 592. Highly Effective Cancer Cell Growth Inhibitory Structural Modifications of Dolastatin 10 |
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