Stereocontrolled Total Synthesis of Biologically Active Natural Products

Hatakeyama, Susumi

doi:10.1248/yakushi.17-00187

Cited by 3 publications

(3 citation statements)

References 107 publications

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“…Arboridinine Kopsia arborea (plant) 5 1 6 2 3 1 6 adunctin B (Dethe and Dherange, 2018) Piper adunctum (plant) 4 1 8 1 3 6 2 3 (±)-deguelin Tephrosia vogelii (plant) 5 1 9 3 2 4 6 2 englerin A (Hatakeyama, 2018) Phyllanthus engleri (plant) 5 1 9 2 6 2 3 1 3 houttuynoid A (Jian et al, 2018) Houttuynia cordata (plant) 5 2 2 3 4 7 2 4 (−)-mucosin (Nolsoe et al, 2018) Reniera mucosa ( This kind of tool would incredibly ease the access to plant natural chemical diversity and should ideally be comprehensive, organized and include data from worldwide plant species, from past to recent studies. Such a globalized database could furthermore be integrated to other ones like genomic, phylogenic, species occurrence, biosynthetic pathway, biological activity, or chemical classification (Allen et al, 2019) allowing researchers to mine the resources and correlate the information, hence empowering all kind of research studies.…”

Section: Discussionmentioning

confidence: 99%

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

Lautie

Russo

Ducrot³

2020

Front. Pharmacol.

166

120

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The screening and testing of extracts against a variety of pharmacological targets in order to benefit from the immense natural chemical diversity is a concern in many laboratories worldwide. And several successes have been recorded in finding new actives in natural products, some of which have become new drugs or new sources of inspiration for drugs. But in view of the vast amount of research on the subject, it is surprising that not more drug candidates were found. In our view, it is fundamental to reflect upon the approaches of such drug discovery programs and the technical processes that are used, along with their inherent difficulties and biases. Based on an extensive survey of recent publications, we discuss the origin and the variety of natural chemical diversity as well as the strategies to having the potential to embrace this diversity. It seemed to us that some of the difficulties of the area could be related with the technical approaches that are used, so the present review begins with synthetizing some of the more used discovery strategies, exemplifying some key points, in order to address some of their limitations. It appears that one of the challenges of natural product-based drug discovery programs should be an easier access to renewable sources of plant-derived products. Maximizing the use of the data together with the exploration of chemical diversity while working on reasonable supply of natural product-based entities could be a way to answer this challenge. We suggested alternative ways to access and explore part of this chemical diversity with in vitro cultures. We also reinforced how important it was organizing and making available this worldwide knowledge in an "inventory" of natural products and their sources. And finally, we focused on strategies based on synthetic biology and syntheses that allow reaching industrial scale supply. Approaches based on the opportunities lying in untapped natural plant chemical diversity are also considered.

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Section: Discussionmentioning

confidence: 99%

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

Lautie

Russo

Ducrot³

2020

Front. Pharmacol.

166

120

View full text Add to dashboard Cite

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“…354–356 In addition, total synthesis routes for various Tir and tirandalydigin (a hybrid of the Tir–Stl family) derivatives became available. 331,357,358…”

Section: Characterized Target Sites Of Rnap and Respective Inhibitorsmentioning

confidence: 99%

“…[354][355][356] In addition, total synthesis routes for various Tir and tirandalydigin (a hybrid of the Tir-Stl family) derivatives became available. 331,357,358 TirA is an inhibitor of RNAP, similar to Stl, and interferes with initialization of transcription and the elongation process. However, its activity is $40 fold less potent than Stl.…”

Section: Reviewmentioning

confidence: 99%