Chapter 5 Alkylating Agents-Epoxides and Lactones

This article describes direct photoalkylation of electron-rich aromatic compounds with diazo compoiunds. C-2 alkylated indoles and pyrroles are obtained with good yields even though the photocatalyst (Ru(bpy)3Cl2) loading is as low as 0.075 mol %. For substrates bearing electron-withdrawing substituents the addition of a catalytic amount of N,N-dimethyl-4-methoxyaniline is required. Both EWG-EWG and EWG-EDG substituted diazo esters are suitable as alkylating agents. The reaction selectivity and mechanistic experiments suggest that carbenes/carbenoid intermediates are not involved in the reaction pathway, instead radical formation is proposed.

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Mechanisms of action of quinone-containing alkylating agents i: NQO1-directed drug development

Frontiers in Bioscience ◽

10.2741/beall ◽

2000 ◽

Vol 5 (1) ◽

pp. d639 ◽

Cited By ~ 30

Author(s):

Howard, D. Beall

Keyword(s):

Drug Development ◽

Alkylating Agents ◽

Mechanisms Of Action

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Faculty Opinions recommendation of Mechanisms of Lymphoma Clearance Induced by High-Dose Alkylating Agents.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.735675980.793567438 ◽

2019 ◽

Author(s):

Varsha Gandhi ◽

Maria Teresa Bertilaccio

Keyword(s):

Alkylating Agents ◽

High Dose

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Hydrogeochemistry of Toxic Elements in Urbanized Geotechnical Systems

Water Quality Research Journal ◽

10.2166/wqrj.1997.030 ◽

1997 ◽

Vol 32 (3) ◽

pp. 523-550

Author(s):

S.N. Volkov

Keyword(s):

Heavy Metals ◽

Toxic Elements ◽

Life Support ◽

Alkylating Agents ◽

Pollution Sources ◽

The Urals

Abstract In urbanized geotechnical systems (UGSs), the majority of problems related to the ecological hydrochemistry of Cd, Pb, Ni and other heavy metals are the result of emergent characteristics of a system as a whole as opposed to individual pollution sources. In petrochemical UGSs, pollution of the environment from compounds containing methylating or alkylating agents results in an increase in the mobility of Cd, Pb, Ni, Cr and As. This process is controlled by environmental and microclimatic factors rather than by pollution sources. Under conditions of predominant dust and element effects, geo-chemically paradoxical associations of Cd with Ni, Mn and Cr can be formed in the main life support media in mining and metallurgical UGSs. Uncontrolled processes of hydrochemical interactions take place in complex multifunctional UGSs, leading to a change in speciation of heavy metals, particularly cadmium. This report is part of a 5-year study of the geotechnical systems in the Urals.

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Recent Progress of Benzimidazole Hybrids for Anticancer Potential

Current Medicinal Chemistry ◽

10.2174/0929867326666190808122929 ◽

2020 ◽

Vol 27 (35) ◽

pp. 5970-6014 ◽

Cited By ~ 3

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.

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Molecular Topological Properties of Alkylating Agents Based Anticancer Drug Candidates Via Some Ve-degree Topological Indices

Current Computer - Aided Drug Design ◽

10.2174/1573409915666190807145908 ◽

2020 ◽

Vol 16 (2) ◽

pp. 190-195 ◽

Cited By ~ 1

Author(s):

Süleyman Ediz ◽

Murat Cancan

Keyword(s):

Anticancer Drugs ◽

Anticancer Drug ◽

Alkylating Agents ◽

Topological Indices ◽

Pharmacological Properties ◽

Topological Properties ◽

Drug Candidates ◽

New Drug ◽

Atom Bond ◽

Dual Target

Background: Reckoning molecular topological indices of drug structures gives the data about the underlying topology of these drug structures. Novel anticancer drugs have been leading by researchers to produce ideal drugs. Materials and Methods: Pharmacological properties of these new drug agents explored by utilizing simulation strategies. Topological indices additionally have been utilized to research pharmacological properties of some drug structures. Novel alkylating agents based anticancer drug candidates and ve-degree molecular topological indices have been introduced recently. Results and Conclusion: In this study we calculate ve-degree atom-bond connectivity, harmonic, geometric-arithmetic and sum-connectivity molecular topological indices for the newly defined alkylating agents based dual-target anticancer drug candidates.

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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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