Abstract
Synthetic approaches to macrosphelide derivatives, based on medicinal chemistry, are summarized. This review contains conventional medicinal chemistry approaches, combinatorial chemistry, fluorous tagging techniques and affinity chromatography preparation. In addition, advances in their apoptosis-inducing activities are also included.
Highlights
As the urgent demand for the development of new drugs increases, rapid innovations in medicinal chemistry, natural product isolation, chemical biology approaches and target protein identification techniques have taken place [1,2,3]
The first derivatization of MS was carried out to determine the exact structure of MSB via oxidation of MSA, as shown in Scheme 1 [11,18]
FO5050, MSA was treated with pyridinium dichlorochromate (PDC) to oxidize the secondary hydroxyl group to determine the absolute structure of MSB
Summary
As the urgent demand for the development of new drugs increases, rapid innovations in medicinal chemistry, natural product isolation, chemical biology approaches and target protein identification techniques have taken place [1,2,3]. New therapeutic agents for cancer patients have been anticipated because most cancer cells are resistant to long-term therapy and are readily mobile through metastasis [4]. For this reason, tremendous efforts have been poured into discovering novel metastasis inhibitors and tumor cell growth inhibitors [5]. MSB shows a strong in vivo immunosuppressant activity equipotent to that of rapamycin or cyclosporine, which are used clinically [15] Based on these basic bioactivities, natural MS isomers [16], and variety of MS derivatives have been synthesized to improve their activity and reveal undiscovered features [17]. A synthetic study to develop MS-related derivatives is discussed
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