Synthetic and Structure-Activity Relationship of Insecticidal Bufadienolides
نویسندگان
چکیده
منابع مشابه
Structure-activity relationship of kahalalide F synthetic analogues.
Kahalalide F (KF) is a natural product currently under phase II clinical trials. Here, we report the solid phase synthesis of 132 novel analogues of kahalalide F and their in vitro activity on a panel of up to 14 cancer cell lines. The structure-activity relationship of these analogues revealed that KF is highly sensitive to backbone stereotopical modification but not to side chain size modific...
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Spicamycin, a nucleoside antibiotic containing fatty acids with a variety of chain lengths (C12-C18), showed potent antitumor activity against human gastric cancer SC-9 and human breast cancer MX-1 in a xenograft model. We have made several semi-synthetic spicamycin analogues (SPMs) which differed in the chain length of the fatty acid moiety, and examined their structure-antitumor activity rela...
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The phytochemistry of the genus Piper (Piperaceae) has been widely studied due to the biological properties of amides from these plants. In this work, we have synthesized and evaluated the toxic effect of 11 amides against the fall armyworm Spodoptera frugiperda larvae. The naturally occurring piperine was also evaluated. The most active amide was N-[3-(3',4'-methylenedioxyphenyl)-2-(E)-propeno...
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Molecular Structure-Affinity Relationship of Bufadienolides and Human Serum Albumin In Vitro and Molecular Docking Analysis
The development of bufadienolides as anti-tumor agents is limited due to poor pharmacokinetic properties regarding drug half-lives and toxicity in vivo. These serious factors might be improved by increasing the drug/albumin-binding ratio. This study therefore investigated the relationship between the structural properties of nine bufadienolides and their affinities for human serum albumin (HSA)...
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ژورنال
عنوان ژورنال: Natural Product Communications
سال: 2014
ISSN: 1934-578X,1555-9475
DOI: 10.1177/1934578x1400900710