Synthesis of Potential Anticancer Agents. III. Nitrogen Mustards Derived from 8-Aminoquinolines1-3

1960 ◽  
Vol 25 (9) ◽  
pp. 1576-1583 ◽  
Author(s):  
ROBERT C. ELDERFIELD ◽  
ERNEST F. LeVON
Keyword(s):  
Anticancer Agents ◽  
Nitrogen Mustards

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.

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

Potential Anticancer Agents.1LXXIX. Aromatic Nitrogen Mustards Derived from Cysteine2

1963 ◽  
Vol 6 (1) ◽  
pp. 43-46 ◽  
Author(s):  
Robert H. Iwamoto ◽  
Edward M. Acton ◽  
Leonard O. Ross ◽  
W. A. Skinner ◽  
B. R. Baker ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Nitrogen Mustards

ChemInform Abstract: POTENTIAL ANTICANCER AGENTS PART 8, NEW AROMATIC AND HETEROAROMATIC NITROGEN MUSTARDS

1973 ◽  
Vol 4 (52) ◽  
pp. no-no
Author(s):  
I. NICULESCU-DUVAZ ◽  
M. ROTARU ◽  
V. FEYNS ◽  
O. MAIOR
Keyword(s):  
Anticancer Agents ◽  
Nitrogen Mustards
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