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Molecules
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Natural Product Synthesis: A Platform for Discovery
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Natural Product Synthesis: A Platform for Discovery

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: closed (30 October 2015) | Viewed by 12961

Special Issue Editor

Prof. Dr. Joshua G. Pierce

E-Mail Website
Guest Editor
Department of Chemistry, North Carolina State University, 2620 Yarbrough Drive, Raleigh, NC 27695, USA
Interests: natural product synthesis; heterocyclic chemistry; medicinal chemistry; chemical biology

Special Issue Information

Dear Colleagues,

In recent years there has been a resurgence in the chemical and biological communities’ interest in complex natural products and their analogs. The discoveries, which emerge from programs invested in the synthesis and biological evaluation of such molecules, range from versatile synthetic methods to new probes for biological pathways to leads for drug discovery. This Special Issue on natural products synthesis will offer an attractive forum to present the chemical and/or biological discoveries resulting from efforts toward the synthesis of natural products. I strongly encourage authors to submit papers for this Special Issue on natural products synthesis, within the scope of Molecules. I hope that the topics covered will reflect the potential and the excitement of natural products chemistry and serve as a collection of representative articles to inspire future discoveries.

Dr. Joshua G. Pierce
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


Keywords

  • natural products
  • heterocycles
  • methods development
  • stereoselectivity
  • probe molecules
  • biological screening

Published Papers (2 papers)

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Research

739 KiB  
Article
Concise Synthesis of Broussonone A
by Hyeju Jo, Minho Choi, Mayavan Viji, Young Hee Lee, Young-Shin Kwak, Kiho Lee, Nam Song Choi, Yeon-Ju Lee, Heesoon Lee, Jin Tae Hong, Mi Kyeong Lee and Jae-Kyung Jung
Molecules 2015, 20(9), 15966-15975; https://doi.org/10.3390/molecules200915966 - 2 Sep 2015
Cited by 15 | Viewed by 6036
Abstract
A concise and expeditious approach to the total synthesis of broussonone A, a p-quinol natural compound, has been developed. The key features of the synthesis include the Grubbs II catalyst mediated cross metathesis of two aromatic subunits, and a chemoselective oxidative dearomatizationin [...] Read more.
A concise and expeditious approach to the total synthesis of broussonone A, a p-quinol natural compound, has been developed. The key features of the synthesis include the Grubbs II catalyst mediated cross metathesis of two aromatic subunits, and a chemoselective oxidative dearomatizationin the presence of two phenol moieties. Especially, optimization associated with the CM reaction of ortho-alkoxystyrenes was also studied, which are known to be ineffective for Ru-catalyzed metathesis reactions under conventional reaction conditions because ortho-alkoxy group could coordinate to the ruthenium center, resulting in the potential complication of catalyst inhibition. Full article
(This article belongs to the Special Issue Natural Product Synthesis: A Platform for Discovery)
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910 KiB  
Article
Synthesis, Biological Activities, and Quantitative Structure–Activity Relationship (QSAR) Study of Novel Camptothecin Analogues
by Dan Wu, Shao-Yong Zhang, Ying-Qian Liu, Xiao-Bing Wu, Gao-Xiang Zhu, Yan Zhang, Wei Wei, Huan-Xiang Liu and An-Liang Chen
Molecules 2015, 20(5), 8634-8653; https://doi.org/10.3390/molecules20058634 - 13 May 2015
Cited by 12 | Viewed by 6643
Abstract
In continuation of our program aimed at the development of natural product-based pesticidal agents, three series of novel camptothecin derivatives were designed, synthesized, and evaluated for their biological activities against T. Cinnabarinus, B. brassicae, and B. xylophilus. All of the [...] Read more.
In continuation of our program aimed at the development of natural product-based pesticidal agents, three series of novel camptothecin derivatives were designed, synthesized, and evaluated for their biological activities against T. Cinnabarinus, B. brassicae, and B. xylophilus. All of the derivatives showed good-to-excellent activity against three insect species tested, with LC50 values ranging from 0.00761 to 0.35496 mmol/L. Remarkably, all of the compounds were more potent than CPT against T. Cinnabarinus, and compounds 4d and 4c displayed superior activity (LC50 0.00761 mmol/L and 0.00942 mmol/L, respectively) compared with CPT (LC50 0.19719 mmol/L) against T. Cinnabarinus. Based on the observed bioactivities, preliminary structure–activity relationship (SAR) correlations were also discussed. Furthermore, a three-dimensional quantitative structure–activity relationship (3D-QSAR) model using comparative molecular field analysis (CoMFA) was built. The model gave statistically significant results with the cross-validated q2 values of 0.580 and correlation coefficient r2 of 0.991 and of 0.993. The QSAR analysis indicated that the size of the substituents play an important in the activity of 7-modified camptothecin derivatives. These findings will pave the way for further design, structural optimization, and development of camptothecin-derived compounds as pesticidal agents. Full article
(This article belongs to the Special Issue Natural Product Synthesis: A Platform for Discovery)
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