Interventionelle Sonografie der Hand

Caravatti, med. Miguel

doi:10.1007/978-3-642-44940-6_10

Cited by 1 publication

(1 citation statement)

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“…169 Semisynthetic modifications of staurosporine via N-alkylation/acylation allowed access to a number of analogs with increased selectivity for PKC. 170 Subsequently, midostaurin, an Nbenzoyl-staurosporine derivative, was found to have in vivo antitumor activity and to inhibit angiogenesis, eventually leading to its development as a therapeutic to treat acute myeloid leukemia ( Figure 6). 171,172 While other indolocarbazole derivatives were developed and showed increased protein kinase selectivity, they did not advance to the clinic due to lack of efficacy.…”

Section: Additional Case Studiesmentioning

confidence: 99%

Fixing the Unfixable: The Art of Optimizing Natural Products for Human Medicine

Yñigez-Gutierrez

Bachmann

2019

J. Med. Chem.

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Molecules isolated from natural sources including bacteria, fungi, and plants are a long-standing source of therapeutics that continue to add to our medicinal arsenal today. Despite their potency and prominence in the clinic, complex natural products often exhibit a number of liabilities that hinder their development as therapeutics, which may be partially responsible for the current trend away from natural product discovery, research, and development. However, advances in synthetic biology and organic synthesis have inspired a new generation of natural product chemists to tackle powerful undeveloped scaffolds. In this Perspective, we will present case studies demonstrating the historical and current focus on making targeted, but significant, changes to natural product scaffolds via biosynthetic gene cluster manipulation, total synthesis, semisynthesis, or a combination of these methods, with a focus on increasing activity, decreasing toxicity, or improving chemical and pharmacological properties.

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Section: Additional Case Studiesmentioning

confidence: 99%