Recent Progress of Benzimidazole Hybrids for Anticancer Potential

2020 ◽  
Vol 27 (35) ◽  
pp. 5970-6014 ◽  
Author(s):  
Md. Jawaid Akhtar ◽  
Mohammad Shahar Yar ◽  
Vinod Kumar Sharma ◽  
Ahsan Ahmed Khan ◽  
Zulphikar Ali ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Alkylating Agents ◽  
American Chemical Society ◽  
Chemical Society ◽  
Benzimidazole Derivatives ◽  
Progressive Development ◽  
Anticancer Properties ◽  
Naturally Occurring ◽  
Nitrogenous Base

This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.

scholarly journals Design and Synthesis of Benzimidazole-Chalcone Derivatives as Potential Anticancer Agents

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3259 ◽  
Author(s):  
Hsieh ◽  
Ko ◽  
Chang ◽  
Kapoor ◽  
Liang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Alkyl Chain ◽  
Biological Activities ◽  
Breast Adenocarcinoma ◽  
Benzimidazole Derivatives ◽  
Design And Synthesis ◽  
Anticancer Properties ◽  
Human Ovarian Carcinoma ◽  
Mcf 7

Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ovarian carcinoma (OVCAR-3) cell lines. Among the 24 synthesized compounds, (2E)-1-(1-(3-morpholinopropyl)-1H-benzimidazol-2 -yl)-3-phenyl-2-propen-1-one) (23a) reduced the proliferation of MCF-7 and OVCAR-3 cell lines demonstrating superior outcomes to those of cisplatin.

Recent Advances on Cytotoxic Sesquiterpene Lactones

2019 ◽  
Vol 24 (36) ◽  
pp. 4355-4361 ◽  
Author(s):  
José Quintana ◽  
Francisco Estévez
Keyword(s):  
Cell Death ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Alkylating Agents ◽  
Structural Requirement ◽  
Naturally Occurring ◽  
Covalent Adducts

Sesquiterpene lactones are naturally occurring compounds that have attracted considerable attention because to their vast array of biological activities. These plant-derived compounds contain the α-methylene-γ- butyrolactone functional group, which is the structural requirement for their pharmacological activities. Many of them exhibit cancer cell cytotoxicity and are promising anticancer agents through multiple mechanisms of action. Sesquiterpene lactones are alkylating agents that form covalent adducts in vivo and inhibit enzymes and key proteins. They are also potent apoptotic inducers in several cancer cells. This kind of cell death is recognized as a property that is useful for identifying anticancer drugs. This review focuses on the advances on cytotoxic sesquiterpene lactones and specifically the signal transduction pathways of cell death triggered in cancer cells.

scholarly journals Cytotoxic Activity of Some Spirooxindole-4H-pyran Derivatives

2019 ◽  
pp. 1-6
Author(s):  
Zeinab Faghih ◽  
Zahra Faghih ◽  
Masoomeh Divar ◽  
Soghra Khabnadideh
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Science Research ◽  
Cytotoxic Activities ◽  
Medical Sciences ◽  
Anticancer Properties ◽  
Cancerous Cell ◽  
Mcf 7

Aims: Isatin is a honored scaffold and one of the most favorable class of heterocyclic systems that possesses many interesting biological activities and well-tolerated in humans. Here a series of fifteen spirooxindole-4H-pyran derivatives containing both isatin and pyran moieties (ICa-ICo) will be examine for their anti-cancer activity. Study Design: Cytotoxic evaluation of some spirooxindole-4H-pyran derivatives in two cancerous cell lines.  Place and Duration of Study: Pharmaceutical Science Research Center and Shiraz Institute for Cancer Research, Medical School in Shiraz University of Medical Sciences, Shiraz, Iran, between June 2018 and July 2019. Methodology: MTT assay was used to evaluate the cytotoxic activities of these compounds. The anticancer properties of the tested compounds were determined using A549 and MCF-7 cell lines. Results: Among the tested compounds ICc, ICd and ICf showed the best cytotoxic activities  against both cancerous cell lines. Compounds ICh and ICj showed desirable cytotoxic activities against A549 cell line. Compound ICb showed desirable cytotoxic activities against MCF-7 cell line. Conclusion: We conclude that the isatin-linked pyran analog can serve as a prototype molecule for further development of a new class of anticancer agents.

scholarly journals The Phylum Bryozoa as a Promising Source of Anticancer Drugs

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 477 ◽  
Author(s):  
Figuerola ◽  
Avila
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Anticancer Properties ◽  
Antitumor Compounds ◽  
Wide Range ◽  
Drug Synthesis ◽  
Low Toxicity ◽  
Promising Source

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, which are filter-feeding, aquatic invertebrates often characterized by a calcified skeleton, are an excellent source of pharmacologically interesting compounds including well-known chemical classes such as alkaloids and polyketides. This review covers the literature for secondary metabolites isolated from marine cheilostome and ctenostome bryozoans that have shown potential as cancer drugs. Moreover, we highlight examples such as bryostatins, the most known class of marine-derived compounds from this animal phylum, which are advancing through anticancer clinical trials due to their low toxicity and antineoplastic activity. The bryozoan antitumor compounds discovered until now show a wide range of chemical diversity and biological activities. Therefore, more research focusing on the isolation of secondary metabolites with potential anticancer properties from bryozoans and other overlooked taxa covering wider geographic areas is needed for an efficient bioprospecting of natural products.

scholarly journals The Understudied Phylum Bryozoa as a Promising Source of Anticancer Drugs

2019 ◽  
Author(s):  
Blanca Figuerola ◽  
Conxita Avila
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Anticancer Properties ◽  
Wide Range ◽  
Drug Synthesis ◽  
Low Toxicity ◽  
Promising Source ◽  
Excellent Source

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, filter-feeding, sessile aquatic invertebrates often characterized by a calcified skeleton, are an excellent source of pharmacologically interesting compounds including well-known chemical classes such as alkaloids and polyketides. This review covers the literature for secondary metabolites isolated from marine cheilostome and ctenostome bryozoans that have shown potential as cancer drugs. Moreover, we highlight examples such as bryostatins, the most known class of marine-derived compounds from this animal phylum, which is advancing through anticancer clinical trials due to their low toxicity and antineoplastic activity. The bryozoan antitumour compounds discovered until now show a wide range of chemical diversity and biological activities. Therefore, more research focusing on the isolation of secondary metabolites with potential anticancer properties from bryozoans and other overlooked taxa covering wider geographic areas is needed for an efficient bioprospecting of natural products.

Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratik Yadav ◽  
Ashish Kumar ◽  
Ismail Althagafi ◽  
Vishal Nemaysh ◽  
Reeta Rai ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
New Drugs ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties

: Tetrahydroquinoline and isoquinoline scaffolds are important class heterocyclic compounds, which is implied for the development of new drugs and diagnostic for therapeutic function. Naturally occurring as well as synthetic tetrahydroquinolines/isoquinolines possess many different biological activities and have been testified as remarkable cytotoxic and potency in human cancer cell lines. Tetrahydroquinoline/isoquinolines based compounds displayed a key role in the development of anticancer drugs or lead molecules and acting through various mechanisms such as cell proliferation, apoptosis, DNA fragmentation, inhibition of tubulin polymerization, induced cell cycle arrest, interruption of cell migration, and modulation. The number of tetrahydroquinoline/isoquinoline derivatives has been reported as potent anticancer agents. Due to promising anticancer activities and wide-ranging properties of these molecules, we have compiled the literature for the synthesis and anticancer properties of various tetrahydroquinolines and isoquinolines. We have reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity a target involved and structural feature responsible for the better activity, so the reader can directly find the detail for designing new anticancer agents.

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