Recent advances (2015-2016) in anticancer hybrids
Nagaraju Kerru1, Parvesh Singh1, Neil Koorbanally1
1School of Chemistry and Physics, University of KwaZulu Natal, P/Bag X54001, Westville, Durban 4000, South Africa.
Abstract:
In spite of the development of a large number of novel anticancer drugs over the years, Cancer remains as a prominent cause of death, worldwide. Numerous drugs that are currently in clinical practice have developed multidrug resistance along with fatal side effects. Therefore, the utilization of single-target therapy is incapable of providing an effective control on the malignant process. Molecular hybridization, involving a combination of two or more pharmacophores of bioactive scaffolds to generate a single molecular architecture with improved affinity and activity, in comparison to their parent molecules, has emerged as a promising strategy in recent drug discovery research. Hybrid anticancer drugs are of great therapeutic interests since they can potentially overcome most of the pharmacokinetic drawbacks encountered with conventional anticancer drugs. Strategically, the design of anticancer drugs involved the blending or linking of an anticancer drug with another anticancer drug or a carrier molecule which can efficiently target cancer cells with improved biological potential. Major advantages of hybrid anticancer drugs involved increased specificity, better patient compliance, and lower side effects along with reduction in chemo-resistance. The successful utilization of this technique in design and synthesis of novel anticancer hybrids has been well illustrated and documented in the literature. The purpose of the present review article will be to provide an emphasis on the recent developments (2015-16) in anticancer hybrids with insights into their structure-activity relationship (SAR) and mechanism of action.
Insights
Molecular hybridization creates novel anticancer drugs by combining multiple pharmacophores. These hybrid anticancer agents offer improved efficacy, reduced side effects, and overcome drug resistance compared to traditional therapies.
Area of Science:
- Drug Discovery and Development
- Medicinal Chemistry
- Oncology
Background:
- Cancer remains a leading cause of death globally, with existing treatments facing limitations like multidrug resistance and severe side effects.
- Single-target therapies are often insufficient for effective cancer control.
- Molecular hybridization, combining multiple bioactive scaffolds, presents a promising strategy to enhance drug affinity and activity.
Purpose of the Study:
- To review recent developments (2015-2016) in anticancer hybrid drug discovery.
- To provide insights into the structure-activity relationship (SAR) of these novel hybrids.
- To explore the mechanisms of action for advanced anticancer hybrids.
Main Methods:
- Literature review focusing on anticancer hybrid research from 2015-2016.
- Analysis of molecular hybridization strategies in anticancer drug design.
- Examination of structure-activity relationship (SAR) data for synthesized hybrids.
Main Results:
- Hybrid anticancer drugs demonstrate potential to overcome pharmacokinetic limitations of conventional agents.
- Key advantages include increased specificity, improved patient compliance, and reduced chemo-resistance.
- Successful design and synthesis of novel anticancer hybrids have been documented.
Conclusions:
- Molecular hybridization is a powerful strategy for developing next-generation anticancer therapeutics.
- Anticancer hybrids offer a multi-pronged approach to combat cancer, addressing resistance and side effects.
- Further research into SAR and mechanisms of action will optimize hybrid drug development.
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