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One-Pot Synthesis of β-Hydroxysulfones and Its Application in the Preparation of Anticancer Drug Bicalutamide

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One-Pot Synthesis of β-Hydroxysulfones and Its …

An efficient one-pot multistep strategy has been developed, comprising auto-oxidative difunctionalization of alkenes, oxidation of sulfides, and a further reduction of peroxides for the synthesis of complex β-hydroxysulfone derivatives from phenthiols and alkenes. This method has several advantageous characteristics, including readily available substrates, low-cost and environmental benign reagents, nontoxic and renewable solvents, and mild reaction conditions. The application of this transformation to the multigram-scale preparation of the anticancer drug bicalutamide is accomplished.

Anticancer Drug Development High Impact List of Articles PPts Journals 958

An efficient one-pot multistep strategy has been developed, comprising auto-oxidative difunctionalization of alkenes, oxidation of sulfides, and a further reduction of peroxides for the synthesis of complex β-hydroxysulfone derivatives from phenthiols and alkenes. This method has several advantageous characteristics, including readily available substrates, low-cost and environmental benign reagents, nontoxic and renewable solvents, and mild reaction conditions. The application of this transformation to the multigram-scale preparation of the anticancer drug bicalutamide is accomplished.

Full Report On 60+ Anticancer Herbs

Natural Product-Based Drug Design and Discovery – Synthesis of anticancer natural ..

Targeted drug delivery systems can directly deliver the payload to the desired site of action without undesired interaction with normal cells. Number of targeted drug delivery systems i.e. use of microfluidics, nanoparticle-based formulations, and use of monoclonal antibodies for anticancer drugs are in the market and many more are in research phase. Successful translation (from bench to bedside) of potential cancer and gene therapies, particularly small interfering RNA (siRNA) delivery, will largely depend on targeted drug delivery strategies. In future, the advancements in these approaches may lead to significant improvements in cancer therapy procedures to avoid risks associated with chemotherapy in these methodologies.

Largazole, which we isolated from a Floridian cyanobacterium, is the most potent natural HDAC inhibitor to date, and in collaboration with Professor Jiyong Hong (Duke University) we described a concise and convergent synthesis (8 steps, 19% overall yield), which allowed its extension to the preparation of a series of analogues. SAR studies revealed that the thiol group is the pharmacophore of the natural product and liberated during protein-assisted thioester hydrolysis to largazole thiol. We determined that largazole inhibits HDACs in vivo, consequently modulates gene expression and thereby shows efficacy in solid tumor xenograft mouse models and bone-forming efficacy in mouse and rabbit models. The dual action of largazole to stimulate bone formation and inhibit bone resorption indicates largazole’s potential as drug lead for bone-related disorders, in addition to its potential as an anticancer drug. We are also evaluating largazole for other disease indications where cellular reprogramming of transcription may be beneficial.

The use of cannabinoids as anticancer agents - …

Actinomycin D (AMD) is an anti-cancer drug, which binds to DNA and inhibits RNA synthesis

Our Anticancer Drug Synthesis Laboratory is located in the state of Michigan, while our Natural Products Laboratory is strategically located in the state of Florida, a region known for its diversity of semitropical flora and its educational and research activities.

A very significant amount of scientific research has been done in the investigation of anticancer properties of various plants - howevermuch work stillneeds to be done.

A new synthesis of substituted acridine-4-carboxylic acids and the anticancer drug N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA)
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    WCRI maintains two laboratories - the Anticancer Drug Synthesis Laboratory and the Natural Products Laboratory.

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    High specificity anticancer pharmacological drug system, drug synthesis, and drug development process

  • Downloads - Drug Discovery Today

    Synthesis and in-vitro evaluation of anti-cancer drug: Synthesis and in-vitro anticancer evaluation of 1-(sub

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Drug discovery tomorrow: how to Catapult ourselves into the future

The synthesized compounds were subjected to the NCI’s disease-oriented human cell lines screening assay to be evaluated for their antitumor activity. The anticancer assays were performed in accordance with the protocol of the Drug Evaluation Branch, NCI, Bethesda [-].

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