Advancements in the Use of Platinum Complexes as Anticancer Agents

Background: The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one of the most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinum compounds associated resistant cancer are some major disadvantages. Objective: With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers have synthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effects with less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinum and newly synthesized complexes, etc. Method: This review emphasizes recent advancements in drug design and development, the mechanism of platinum (II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents. Conclusion: In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen as scientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-target effects.

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Potential of Anti-Cancer Activity of Secondary Metabolic Products from Marine Fungi

Journal of Fungi ◽

10.3390/jof7060436 ◽

2021 ◽

Vol 7 (6) ◽

pp. 436

Author(s):

Efaq Noman ◽

Muhanna Mohammed Al-Shaibani ◽

Muhammed Adnan Bakhrebah ◽

Reyad Almoheer ◽

Mohammed Al-Sahari ◽

...

Keyword(s):

Anticancer Activity ◽

Cancer Cells ◽

Anticancer Agents ◽

Marine Fungi ◽

Metabolic Process ◽

Anticancer Compounds ◽

Current Review ◽

Anti Cancer ◽

Metabolic Products ◽

Available Information

The promising feature of the fungi from the marine environment as a source for anticancer agents belongs to the fungal ability to produce several compounds and enzymes which contribute effectively against the cancer cells growth. L-asparaginase acts by degrading the asparagine which is the main substance of cancer cells. Moreover, the compounds produced during the secondary metabolic process acts by changing the cell morphology and DNA fragmentation leading to apoptosis of the cancer cells. The current review has analyed the available information on the anticancer activity of the fungi based on the data extracted from the Scopus database. The systematic and bibliometric analysis revealed many of the properties available for the fungi to be the best candidate as a source of anticancer drugs. Doxorubicin, actinomycin, and flavonoids are among the primary chemical drug used for cancer treatment. In comparison, the most anticancer compounds producing fungi are Aspergillus niger, A. fumigatus A. oryzae, A. flavus, A. versicolor, A. terreus, Penicillium citrinum, P. chrysogenum, and P. polonicum and have been used for investigating the anticancer activity against the uterine cervix, pancreatic cancer, ovary, breast, colon, and colorectal cancer.

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Current developments in the Pyran-Based Analogues as Anticancer Agents

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621666211119090302 ◽

2021 ◽

Vol 21 ◽

Author(s):

Parul Grover ◽

Monika Bhardwaj ◽

Lovekesh Mehta ◽

Garima Kapoor ◽

Pooja A. Chawla

Keyword(s):

Anticancer Agents ◽

Biological Activities ◽

Wide Spectrum ◽

Anticancer Compounds ◽

Appropriate Treatment ◽

Anti Cancer ◽

Privileged Structure ◽

Different Types

: Heterocyclic compounds offer an enormous area for new lead molecules for drug discovery. Till today, efforts are being continuously made to find appropriate treatment for the management of the deadly disease of cancer. Amongst the large number of heterocycles that are found in nature, heterocycles having oxygen obtained noteworthy attention due to their distinctive and pharmacological activities.‘Pyran’ is one of the most significant non-aromatic, six-membered ring composed of one oxygen atom and five carbon atoms. It is considered a privileged structure since pyran and its related derivatives exhibit a wide spectrum of biological activities. Pyran derivatives are found to have excellent anti-cancer properties against various types of cancer. The present review focussed on the current advances in different types of pyran-based derivatives as anti-cancer agents. Various in-vitro (cell based testing), in-vivo (animal based testing) models as well as molecular docking along with results are also covered. A subsection describing briefly natural pyran containing anticancer compounds is also incorporated in the review.

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Synthesis and anti-cancer activities of a water soluble gold(III) porphyrin

Journal of Porphyrins and Phthalocyanines ◽

10.1142/s1088424615500236 ◽

2015 ◽

Vol 19 (01-03) ◽

pp. 398-403 ◽

Cited By ~ 12

Author(s):

Aaron D. Lammer ◽

Melissa E. Cook ◽

Jonathan L. Sessler

Keyword(s):

Anticancer Agents ◽

Ovarian Cancer Cell ◽

Ovarian Cancer Cell Line ◽

Aqueous Media ◽

Cancer Cell Line ◽

Aqueous Solubility ◽

Water Soluble ◽

Physiological Conditions ◽

Anti Cancer

Gold(III) compounds continue to be explored for their potential utility as anticancer agents. A recognized limitation is the reactivity of gold(III), which is typically reduced to the more labile gold(I) state under physiological conditions. The use of porphyrins can overcome this problem. However, to date the stabilization provided by the use a strongly chelating porphyrin is offset by the poor solubility of the resulting complex in aqueous media. In this work, we describe the synthesis and in vitro anti-cancer activity of a gold(III)porphyrin complex with relatively good aqueous solubility. As judged from standard antiproliferation assays, this complex displays an IC50 of 9 μM for the A2780 human ovarian cancer cell line. This is a higher level of potency than displayed by two related control systems.

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Enhanced anti-cancer efficacy to cancer cells by doxorubicin loaded water-soluble amino acid-modified β-cyclodextrin platinum complexes

Journal of Inorganic Biochemistry ◽

10.1016/j.jinorgbio.2014.03.012 ◽

2014 ◽

Vol 137 ◽

pp. 31-39 ◽

Cited By ~ 6

Author(s):

Mei-Xia Zhao ◽

Meng Zhao ◽

Er-Zao Zeng ◽

Yang Li ◽

Jin-Ming Li ◽

...

Keyword(s):

Amino Acid ◽

Cancer Cells ◽

Platinum Complexes ◽

Water Soluble ◽

Anti Cancer

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Oxazole-Based Compounds As Anticancer Agents

Current Medicinal Chemistry ◽

10.2174/0929867326666181203130402 ◽

2020 ◽

Vol 26 (41) ◽

pp. 7337-7371 ◽

Cited By ~ 3

Author(s):

Maria A. Chiacchio ◽

Giuseppe Lanza ◽

Ugo Chiacchio ◽

Salvatore V. Giofrè ◽

Roberto Romeo ◽

...

Keyword(s):

Cancer Research ◽

Drug Discovery ◽

Anticancer Agents ◽

Heterocyclic Compounds ◽

Chemical Diversity ◽

Biologically Active ◽

New Drugs ◽

The Core ◽

Anti Cancer ◽

Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

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Diverse thiophenes as scaffolds in anti-cancer drug development: A concise review

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666201202113333 ◽

2020 ◽

Vol 20 ◽

Author(s):

Neha V. Bhilare ◽

Pratibha B. Auti ◽

Vinayak S. Marulkar ◽

Vilas J. Pise

Keyword(s):

Drug Development ◽

Anticancer Agents ◽

Heterocyclic Ring ◽

Biologically Active Compounds ◽

Biologically Active ◽

Cancer Drug ◽

Active Compounds ◽

Natural Origin ◽

Concise Review ◽

Anti Cancer

: Thiophenes are one among the abundantly found heterocyclic ring systems in many biologically active compounds. Moreover various substituted thiophenes exert numerous pharmacological actions on account of their isosteric resemblance with compounds of natural origin thus rendering them with diverse actions like antibacterial, antifungal, antiviral, anti-inflammatory, analgesic, antiallergic, hypotensives etc.. In this review we specifically explore the chemotherapeutic potential of variety of structures consisting of thiophene scaffolds as prospective anticancer agents.

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Cytotoxic Activity and DNA Binding Property of New Aminopyrimidine Derivatives

Letters in Drug Design & Discovery ◽

10.2174/1570180816666190712102119 ◽

2020 ◽

Vol 17 (5) ◽

pp. 640-654

Author(s):

Hamidreza Akrami ◽

Bibi Fatemeh Mirjalili ◽

Omidreza Firuzi ◽

Azadeh Hekmat ◽

Ali Akbar Saboury ◽

...

Keyword(s):

Cell Lines ◽

Anticancer Agents ◽

Lymphoblastic Leukemia ◽

Cd Spectroscopy ◽

Myelogenous Leukemia ◽

Breast Adenocarcinoma ◽

Binding Property ◽

Anticancer Compounds ◽

Calf Thymus ◽

Dna Binding Property

Background: Chromene and anilinopyrimidine heterocyclics are attractive anticancer compounds that have inspired many researchers to design novel derivatives bearing improved anticancer activity. Methods: A series of pyrimidine-fused benzo[f]chromene derivatives 6a-x were synthesized as anticancer hybrids of 1H-benzo[f]chromenes and anilinopyrimidines. The inhibitory activity of the synthesized compounds 6a-x against cell viability of human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (MOLT-4) and human breast adenocarcinoma (MCF-7) cell lines was evaluated using MTT assay. The interaction of the most promising compound with calf-thymus DNA was also studied using spectrometric titrations and Circular Dichroism (CD) spectroscopy. Results: Most compounds showed promising activity against tested cell lines. Among them, 2,4- dimethoxyanilino derivative 6g exhibited the best profile of activity against tested cell lines (IC50s = 1.6-6.1 μM) with no toxicity against NIH3T3 normal cell (IC50 >200 μM). The spectrometric studies exhibited that compound 6g binds to DNA strongly and may change DNA conformation significantly, presumably via a groove binding mechanism. Conclusion: The results of this study suggest that the prototype compound 6g can be considered as a novel lead compound for the design and discovery of novel anticancer agents.

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Nitrogen Mustards as Alkylating Agents: A Review on Chemistry, Mechanism of Action and Current USFDA Status of Drugs

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190305141458 ◽

2019 ◽

Vol 19 (9) ◽

pp. 1080-1102 ◽

Cited By ~ 5

Author(s):

Ghansham S. More ◽

Asha B. Thomas ◽

Sohan S. Chitlange ◽

Rabindra K. Nanda ◽

Rahul L. Gajbhiye

Keyword(s):

Side Effects ◽

Mechanism Of Action ◽

Anticancer Agents ◽

Nitrogen Mustard ◽

Alkylating Agents ◽

Cross Linking ◽

Nitrogen Mustards ◽

Information Leaflets ◽

Anti Cancer ◽

Approved Drugs

Background & Objective: :Nitrogen mustard derivatives form one of the major classes of anti-cancer agents in USFDA approved drugs list. These are polyfunctional alkylating agents which are distinguished by a unique mechanism of adduct formation with DNA involving cross-linking between guanine N-7 of one strand of DNA with the other. The generated cross-linking is irreversible and leads to cell apoptosis. Hence it is of great interest to explore this class of anticancer alkylating agents.Methods::An exhaustive list of reviews, research articles, patents, books, patient information leaflets, and orange book is presented and the contents related to nitrogen mustard anti-cancer agents have been reviewed. Attempts are made to present synthesis schemes in a simplified manner. The mechanism of action of the drugs and their side effects are also systematically elaborated.Results::This review provides a platform for understanding all aspects of such drugs right from synthesis to their mechanism of action and side effects, and lists USFDA approved ANDA players among alkylating anticancer agents in the current market.Conclusion: :Perusing this article, generic scientists will be able to access literature information in this domain easily to gain insight into the nitrogen mustard alkylating agents for further ANDA development. It will help the scientific and research community to continue their pursuit for the design of newer and novel heterocyclic alkylating agents of this class in the coming future.

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Multi-Targeting Anticancer Agents: Rational Approaches, Synthetic Routes and Structure Activity Relationship

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190118120708 ◽

2019 ◽

Vol 19 (7) ◽

pp. 842-874 ◽

Cited By ~ 6

Author(s):

Harbinder Singh ◽

Nihar Kinarivala ◽

Sahil Sharma

Keyword(s):

Anticancer Agents ◽

Cancer Drug ◽

Design And Synthesis ◽

Cancer Drug Discovery ◽

Dual Targeting ◽

Structure Activity ◽

Anti Cancer ◽

Dual Inhibitors ◽

Recent Trends ◽

Synthetic Routes

We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. The simultaneous interruption of two or more targets has improved the therapeutic efficacy as compared to the specific targeted based therapy. In this review, six types of dual targeting agents along with some interesting strategies used for their design and synthesis are discussed. Their pharmacology with various types of the molecular interactions within their specific targets has also been described. This assemblage will reveal the recent trends and insights in front of the scientific community working in dual inhibitors and help them in designing the next generation of multi-targeted anti-cancer agents.

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