Abstract
Novel hexacyclic cage-like hybrid heterocycles have been synthesized in excellent yields employing a relatively less explored non-stabilized azomethine ylides derived from acenaphthenequinone and tyrosine with functionalized dipolarophiles using [3 + 2] cycloaddition strategy. The synthesized hexacyclic cage-like hybrid heterocycles were characterized by spectroscopic analysis. Following the physical characterization, these cage-like hybrid heterocycles were tested for their biological activity by means of different cancer (A549 and Jurkat cells) and non-cancer (BRL-3A and PCS-130) in vitro cell culture systems. The results of the study under tested concentrations (up to 100 μM) indicated that these compounds are not affecting any viability to the cell growth of non-cancer cells, while providing significant anticancer activity against both of the cancer cells. Further analysis of in-depth mechanistic study for the cell death indicated that these compounds are exhibiting late apoptosis or early necrosis pathway to the cells where it is operated by the induction of caspases.
Highlights
Cancer is a disease that causes an abnormal growth of cells to the tissues, called a tumor, where the cells lose their normal functions and when it spreads to the other parts of the body that can eventually lead to death
As a part of our research work directed towards the development of novel anticancer agents anticancer agents based on the ability to block cell proliferation and/or to induce apoptosis, we based on the ability to block cell proliferation and/or to induce apoptosis, we recently reported recently reported the synthesis and apoptotic inducing properties of highly functionalized the synthesis and apoptotic inducing properties of highly functionalized pyrrolidine heterocyclic pyrrolidine heterocyclic hybrids Figure 1 [15,16]
[20] with with a relatively less explored azomethine ylide ylide derived derived from acenaphthenequinone acenaphthenequinone and and tyrosine tyrosine afforded afforded the the novel novel hexacyclic hexacyclic cage-like hybrid heterocycles
Summary
Cancer is a disease that causes an abnormal growth of cells to the tissues, called a tumor, where the cells lose their normal functions and when it spreads to the other parts of the body (metastasis) that can eventually lead to death. The number of cancer diagnosed patients are increasing, as it was about 14.1 million during the year 2012 and is expected to be projected to 21.6 million by the year 2030 [2]. Considering the significant increase in the number of cancer patients every year, the quest for the early diagnosis and safe treatment modalities are being developed by the researchers as the currently available methods are not up to their mark [3,4]. It was found in recent years that the apoptosis pathway plays a key role in the degradation of cancer cells and in that way, a majority of antitumor
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