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Synthesis, biological evaluation, and molecular docking studies of cinnamic acyl 1,3,4-thiadiazole amide derivatives as novel antitubulin agents.
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Based on the preliminary results, compound 10e with potent inhibitory activity in tumor growth may be a potential anticancer agent.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2012-02-01. It has received 75 citations till now. The article focuses on the topics: Tubulin Modulators & Docking (molecular).read more
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1,3,4-Thiadiazole: Synthesis, Reactions, and Applications in Medicinal, Agricultural, and Materials Chemistry
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Thiadiazole-a promising structure in medicinal chemistry.
TL;DR: This Minireview, thiadiazoles are summarized according to their therapeutic potential, highlighting the versatility of this scaffold in medicinal chemistry and giving a brief introduction to their synthesis and diverse biological activities.
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Recent advances of cytotoxic chalconoids targeting tubulin polymerization: Synthesis and biological activity.
Hassan Mirzaei,Saeed Emami +1 more
TL;DR: This review focused on the recently reported tubulin polymerization inhibitors from chalcone origin and related synthetic compounds, and their detailed synthetic methods and biological activities.
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Phenylpropanoids and its derivatives: biological activities and its role in food, pharmaceutical and cosmetic industries.
TL;DR: This review has presented the current knowledge on the biosynthesis, occurrence, biological activities of phenylpropanoids and their derivatives, along with the mechanism of action and their potential applications in various industries.
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1,3,4-Trisubstituted pyrazole analogues as promising anti-inflammatory agents.
TL;DR: The cyclooxygenase (COX) enzyme inhibitor activity of selected compounds, which are the excellent anti-inflammatory activities in carrageenan-induced paw edema model, was investigated in vitro COX inhibition assay and molecular docking study further helped in supporting the observed activity.
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Insight into tubulin regulation from a complex with colchicine and a stathmin-like domain
Raimond B. G. Ravelli,Benoît Gigant,Patrick A. Curmi,Isabelle Jourdain,Sylvie Lachkar,André Sobel,Marcel Knossow +6 more
TL;DR: Changes in the subunits of tubulin as it switches from its straight conformation to a curved one correlate with the loss of lateral contacts and provide a rationale for the rapid microtubule depolymerization characteristic of dynamic instability.
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Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4
TL;DR: The African treeCombretum caffrum (Combretaceae) has been found to contain a powerful inhibitor of tubulin polymerization (IC502–3 μM), the growth of murine lymphocytic leukemia and human colon cancer cell lines.
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Chalcones: an update on cytotoxic and chemoprotective properties.
Mei-Lin Go,X. Wu,X. L. Liu +2 more
TL;DR: The thiol reactivity of chalcones is likely to contribute to both cytotoxic and chemoprotective properties of these compounds.
Journal Article
Bioactivities of chalcones.
TL;DR: In this article, the authors outline the different bioactivities of a variety of chalcones and describe the cytotoxic, anticancer, chemopreventative and mutagenic properties of a number of CHs followed by an account of various CHs as antimicrobial agents.
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Chalcones and flavonoids as anti-tuberculosis agents.
TL;DR: A hydrophobic substituent on one aromatic ring, and a hydrogen-bonding group on the other aromatic ring resulted in increased anti-TB activity of the chalcones and chalcone-like compounds.