scholarly journals The PIFA-initiated oxidative cyclization of 2-(3-butenyl)quinazolin-4(3H)-ones – an efficient approach to 1-(hydroxymethyl)-2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-ones

2021 ◽  
Vol 17 ◽  
pp. 2787-2794
Author(s):  
Alla I Vaskevych ◽  
Nataliia O Savinchuk ◽  
Ruslan I Vaskevych ◽  
Eduard B Rusanov ◽  
Oleksandr O Grygorenko ◽  
...  
Keyword(s):  
Natural Product ◽  
Oxidative Cyclization ◽  
Efficient Approach ◽  
Compound Libraries ◽  
Naturally Occurring

A regioselective method for the synthesis of 1-(hydroxymethyl)-2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-ones – close structural analogs of naturally occurring vasicinone alkaloids – is described. The procedure is based on PIFA-initiated oxidative 5-exo-trig cyclization of 2-(3-butenyl)quinazolin-4(3Н)-ones, in turn prepared by thermal cyclocondensation of the corresponding 2-(pent-4-enamido)benzamides. The products obtained have a good natural product likeness (NPL) score and therefore can be useful for the design of natural product-like compound libraries.

scholarly journals New Pharmacological Opportunities for Betulinic Acid

Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 8-19 ◽  
Author(s):  
José Ríos ◽  
Salvador Máñez
Keyword(s):  
Metabolic Syndrome ◽  
Natural Product ◽  
Betulinic Acid ◽  
Therapeutic Potential ◽  
Present Review ◽  
Antitumor Effects ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Wide Range ◽  
Birch Trees

AbstractBetulinic acid is a naturally occurring pentacyclic lupane-type triterpenoid usually isolated from birch trees, but present in many other botanical sources. It is found in different plant organs, both as a free aglycon and as glycosyl derivatives. A wide range of pharmacological activities has been described for this triterpenoid, including antiviral and antitumor effects. In addition, several other interesting properties have been identified in the fields of immunity and metabolism, namely antidiabetic, antihyperlipidemic, and anti-inflammatory activities. Taken together, these latter three properties make betulinic acid a highly interesting prospect for treating metabolic syndrome. The present review focuses on the therapeutic potential of this agent, along with several of its semisynthetic derivatives, which could open new frontiers in the use of natural product-based medicines.

scholarly journals Total Syntheses of Pladienolide-Derived Spliceosome Modulators

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5938
Author(s):  
Jaehoon Sim ◽  
Eunbin Jang ◽  
Hyun Jin Kim ◽  
Hongjun Jeon
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Structural Features ◽  
Synthetic Approach ◽  
Synthetic Analog ◽  
Phase I Clinical Trials ◽  
Total Syntheses ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Synthetic Approaches

Pladienolides, an emerging class of naturally occurring spliceosome modulators, exhibit interesting structural features, such as highly substituted 12-membered macrocycles and epoxide-containing diene side chains. The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synthetic analog of this natural product class, which is currently under Phase I clinical trials. Since its isolation in 2004 and the first total synthesis in 2007, a dozen total syntheses and synthetic approaches toward the pladienolide class have been reported to date. This review focuses on the eight completed total syntheses of naturally occurring pladienolides or their synthetic analogs, in addition to a synthetic approach to the main framework of the natural product.

Versuche zur Synthese natürlich vorkommender prenylierter Naphthalinderivate. Nachweis eines neuen Prenylnaphthochinon- derivates in Galium mollugo / Synthesis of Naturally Occurring Prenylated Naphthalene Derivates. Isolation of a New Prenylnaphthoquinone from Galium mollugo

1982 ◽  
Vol 37 (5-6) ◽  
pp. 354-362 ◽  
Author(s):  
Lutz Heide ◽  
Eckhard Leistner
Keyword(s):  
Natural Product ◽  
Root System ◽  
Spectroscopic Methods ◽  
Naphthalene Derivatives ◽  
Naturally Occurring

AbstractSeveral prenylated naphthalene derivatives were synthesized and characterized by spectroscopic methods. One of these compounds, 2-methoxycarbonyl-3-prenyl-1,4-naphthoquinone, was detected as a new natural product in the root system of Galium mollugo L. This new natural product is likely to be related to the biosynthesis of mollugin and anthraquinones.

A Practical and Efficient Approach to the Preparation of Bioactive Natural Product Wogonin

2017 ◽  
Vol 21 (2) ◽  
pp. 171-176 ◽  
Author(s):  
Tinghan Li ◽  
Tianwei Weng ◽  
Jubo Wang ◽  
Zhihui Wei ◽  
Lu Zhao ◽  
...  
Keyword(s):  
Natural Product ◽  
Efficient Approach ◽  
Bioactive Natural Product

scholarly journals Harnessing Natural Product Diversity for Fluorophore Discovery: Naturally Occurring Fluorescent Hydroxyanthraquinones from the Marine Crinoid Pterometra venusta

2018 ◽  
Vol 81 (12) ◽  
pp. 2750-2755 ◽  
Author(s):  
A. Jonathan Singh ◽  
Alexander P. Gorka ◽  
Heidi R. Bokesch ◽  
Antony Wamiru ◽  
Barry R. O’Keefe ◽  
...  
Keyword(s):  
Natural Product ◽  
Product Diversity ◽  
Naturally Occurring

scholarly journals A Phenotarget Approach for Identifying an Alkaloid Interacting with the Tuberculosis Protein Rv1466

Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 149 ◽  
Author(s):  
Yan Xie ◽  
Yunjiang Feng ◽  
Angela Di Capua ◽  
Tin Mak ◽  
Garry W. Buchko ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Mycobacterium Tuberculosis ◽  
Drug Discovery ◽  
Natural Product ◽  
Covalent Bond ◽  
Pure Compound ◽  
Active Components ◽  
Ligand Complex ◽  
Mycobacterium Tuberculosis H37rv ◽  
Compound Libraries

In recent years, there has been a revival of interest in phenotypic-based drug discovery (PDD) due to target-based drug discovery (TDD) falling below expectations. Both PDD and TDD have their unique advantages and should be used as complementary methods in drug discovery. The PhenoTarget approach combines the strengths of the PDD and TDD approaches. Phenotypic screening is conducted initially to detect cellular active components and the hits are then screened against a panel of putative targets. This PhenoTarget protocol can be equally applied to pure compound libraries as well as natural product fractions. Here we described the use of the PhenoTarget approach to identify an anti-tuberculosis lead compound. Fractions from Polycarpa aurata were identified with activity against Mycobacterium tuberculosis H37Rv. Native magnetic resonance mass spectrometry (MRMS) against a panel of 37 proteins from Mycobacterium proteomes showed that a fraction from a 95% ethanol re-extraction specifically formed a protein-ligand complex with Rv1466, a putative uncharacterized Mycobacterium tuberculosis protein. The natural product responsible was isolated and characterized to be polycarpine. The molecular weight of the ligand bound to Rv1466, 233 Da, was half the molecular weight of polycarpine less one proton, indicating that polycarpine formed a covalent bond with Rv1466.

scholarly journals Isolation and synthesis of cryptosanguinolentine (isocryptolepine), a naturally-occurring bioactive indoloquinoline alkaloid

RSC Advances ◽  
2020 ◽  
Vol 10 (32) ◽  
pp. 18978-19002
Author(s):  
Elida N. Thobokholt ◽  
Enrique L. Larghi ◽  
Andrea B. J. Bracca ◽  
Teodoro S. Kaufman
Keyword(s):  
Natural Product ◽  
Naturally Occurring

The isolation and properties of the heterocycle are detailed and the diversity of chemical approaches toward the natural product are systematically ordered and reviewed.

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