3-D QSAR CoMFA study of nitrogen mustards possessing new chemical entities as possible anticancer agents

2006 ◽  
Vol 68 (3) ◽  
pp. 323 ◽  
Author(s):  
V Murugan ◽  
RM Anand ◽  
K Sumathi ◽  
SV Sharma
Keyword(s):  
Anticancer Agents ◽  
Nitrogen Mustards ◽  
New Chemical Entities ◽  
Comfa Study

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

2019 ◽  
Vol 19 (9) ◽  
pp. 1080-1102 ◽  
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.

Development of Natural Bioactive Alkaloids: Anticancer perspective

2021 ◽  
Vol 21 ◽  
Author(s):  
Ashish Patel ◽  
Ravi Vanecha ◽  
Jay Patel ◽  
Divy Patel ◽  
Umang Shah ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Low Cost ◽  
Chemical Compounds ◽  
Cost Effective ◽  
Drug Discovery And Development ◽  
Anticancer Properties ◽  
Antimetastatic Activity ◽  
New Chemical Entities

: Cancer is a frightful disease that still poses a 'nightmare' worldwide, causing millions of casualties annually due to one of the human race's most significant healthcare challenges that requires a pragmatic treatment strategy. However, plants and plant-derived products revolutionize the field as they are quick, cleaner, eco-friendly, low-cost, effective, and less toxic than conventional treatment methods. Plants are repositories for new chemical entities and have a promising cancer research path, supplying 60% of the anticancer agents currently used. Alkaloids are important chemical compounds that serve as a rich reservoir for drug discovery and development. However, some alkaloids derived from natural herbs display anti-proliferation and antimetastatic activity on different forms of cancer, both in vitro and in vivo. Alkaloids have also been widely formulated as anticancer medications, such as camptothecin and vinblastine. Still, more research and clinical trials are required before final recommendations can be made on specific alkaloids. This review focuses on the naturally-derived bioactive alkaloids with prospective anticancer properties based on the information in the literature.

Synthesis and evaluation of new benzimidazole derivatives with hydrazone moiety as anticancer agents

2018 ◽  
Vol 43 (2) ◽  
pp. 151-158 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Begüm Nurpelin Sağlık ◽  
Cankız Mina Ardıç ◽  
Yusuf Özkay ◽  
Özlem Atlı
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Point Of View ◽  
Current Therapy ◽  
Benzimidazole Derivatives ◽  
Anticancer Activities ◽  
New Chemical Entities ◽  
Nih 3T3 ◽  
Mcf 7

Abstract Objectives: Cancer is one of the leading causes of death throughout the world. Current therapy options suffer from the major limitations of side effects and drug resistance. Thus, continuing search for newer and safer anticancer drugs remains critically important. From this point of view, in the present study benzimidazole-hydrazone derivatives were synthesized by aiming at the identification of new chemical entities as potent anticancer agents. Material and methods: A series of 12 new compounds of 4-(5(6)-substituted-1H-benzimidazol-2-yl)-N′thiophen/furan-2-yl-methylene) benzohydrazide derivatives were synthesized. The structures of the obtained compounds were elucidated using by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses. In vitro cytotoxic activity of the compounds against A549, MCF-7 and NIH/3T3 cell lines was evaluated by MTT assay. Results: Among the tested compounds, compound 3e showed higher cytotoxicity against MCF-7 human breast cancer cells when compared with cisplatin. Also, it has lower cytotoxicty against healthy cell line, NIH/3T3. Conclusions: It was determined that compound 3e showed inhibition towards MCF-7. Considering the substituent effect on cytotoxic activity, compound 3e bearing 2-methylthiophene has attracted attention with its higher anticancer activities.

Discovery of steroidal lactam conjugates of POPAM-NH2 with potent anticancer activity

2020 ◽  
Vol 12 (1) ◽  
pp. 19-35 ◽  
Author(s):  
Dimitrios Trafalis ◽  
Panagiotis Dalezis ◽  
Elena Geromichalou ◽  
Sofia Sagredou ◽  
Eleni Sflakidou ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Alkylating Agents ◽  
Experimental Models ◽  
The Novel ◽  
Nitrogen Mustards ◽  
Experimental Systems ◽  
High Antitumor Activity

Aim: Steroidal prodrugs of nitrogen mustards such as estramustine and prednimustine have proven effective anticancer agents in clinical use since the 1970s. In this work, we aimed to develop steroidal prodrugs of the novel nitrogen mustard POPAM-NH2. POPAM-NH2 is a melphalan analogue that was coupled with three different steroidal lactams. Methodology: The new conjugates were preclinically tested for anticancer activity against nine human and one rodent cancer experimental models, in vitro and in vivo. Results & conclusion: All the steroidal alkylators showed high antitumor activity, in vitro and in vivo, in the experimental systems tested. Moreover, these hybrid compounds showed by far superior anticancer activity compared with the alkylating agents, melphalan and POPAM-NH2.

Potential anticancer agents. IV. Nitrogen mustards of methylbenzoic acids

1968 ◽  
Vol 11 (3) ◽  
pp. 500-503 ◽  
Author(s):  
I. Niculescu-Duvaz ◽  
Michaela Ionescu ◽  
A. Cambanis ◽  
M. Vitan ◽  
V. Feyns
Keyword(s):  
Anticancer Agents ◽  
Nitrogen Mustards

Synthesis of Potential Anticancer Agents. XIX. Nitrogen Mustards from 7-Hydroxycoumarin Derivatives

1967 ◽  
Vol 10 (5) ◽  
pp. 921-923 ◽  
Author(s):  
Robert C. Elderfield ◽  
A. C. Mehta
Keyword(s):  
Anticancer Agents ◽  
Nitrogen Mustards

Recent Advances in the Development of Pyrazolopyridines as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Xiaotong Gu ◽  
Shutao Ma
Keyword(s):  
Anticancer Activity ◽  
21St Century ◽  
Malignant Tumor ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Biological Processes ◽  
Health It ◽  
Recent Advances ◽  
New Chemical Entities

: Cancer, especially malignant tumor, is a serious threat to people's life and health. It is recognized as an enormous challenge in the 21st century. Continuous efforts are needed to overcome this problem. Pyrazolopyridine nucleus, similar in structure to purine, shows a variety of biological activities, which is mainly attributed to the antagonistic nature towards the natural purines in many biological processes. This has aroused enormous attention for many researchers. At present, a large number of new chemical entities containing pyrazolopyridine nucleus have been found as anticancer agents. In this review we summarize novel pyrazolopyridine-containing derivatives with biological activities. Furthermore, we outline the relationships between the structures of variously modified pyrazolopyridines and their anticancer activity.

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