From Natural Sources to Synthetic Derivatives: The Allyl Motif as a Powerful Tool for Fragment-Based Design in Cancer Treatment

Abstract

Since the beginning of history, natural products have been an abundant source of bioactive molecules for the treatment of different diseases, including cancer. Many allyl derivatives, which have shown anticancer activity both in vitro and in vivo in a large number of cancers, are bioactive molecules found in garlic, cinnamon, nutmeg, or mustard. In addition, synthetic products containing allyl fragments have been developed showing potent anticancer properties. Of particular note is the allyl derivative 17-AAG, which has been evaluated in Phase I and Phase II/III clinical trials for the treatment of multiple myeloma, metastatic melanoma, renal cancer, and breast cancer. In this Perspective, we compile extensive literature evidence with descriptions and discussions of the most recent advances in different natural and synthetic allyl derivatives that could generate cancer drug candidates in the near future.

Exploring the Structural Importance of the C3═C4 Double Bond in Plant Alkaloids Harmine and Harmaline on Their Binding Interactions with Hemoglobin

“…Natural products have long been an important source of therapeutic drugs, which promotes new approaches in organic synthesis . Several recent investigations have reported the molecular interaction between protein and ligand through advanced multispectroscopic methods. − The plant alkaloids, harmine and harmaline have different health-beneficial activities such as antioxidant, anti-inflammatory, antimicrobial, and antitumor activities.…”

Organoselenium Compounds in Catalysis

“…Including its important role in medicinal chemistry, [37][38][39][40][41] organoselenium compounds not only show interesting chemical properties, but also their use in catalysis is very relevant and…”

“…Including its important role in medicinal chemistry, [37][38][39][40][41] organoselenium compounds not only show interesting chemical properties, but also their use in catalysis is very relevant and supported by copious bibliography. [42][43][44][45][46][47] In fact, the use of organoselenium compounds as promoters in a number of organic reactions has been established.…”

Selenium-analogs based on natural sources as cancer-associated carbonic anhydrase isoforms IX and XII inhibitors

“…It is also found in benzyl allylic derivatives present in several plants such as cloves, curcuma, anise, or parsley. 31 On the other hand, the active propargylic fragment can be found in natural marine products such as viridamide (isolated from cyanobacteria) and duryne (metabolite produced by one type of marine sponge). The other part of the molecule, which ought to be released in the form of carboxylic acid, are carbo- and hetero-cycles derivatives and NSAIDs.…”