Synthesis of 5-Fluorouracil Derivatives as Possible Mutual Prodrugs with Meloxicam and Ibuprofen for Targeting Cancer Tissues

Dakhel, Zainab A.H.

doi:10.31351/vol20iss2pp9-18

Cited by 3 publications

(1 citation statement)

References 15 publications

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“…Antimetabolites are chemotherapeutic drugs that bind to macromolecules like DNA and RNA, and interfere with vital metabolic procedures. This group of drugs constitute a class of substances that interfere with the normal functioning of cells (Al-hoshary and Zalzala 2023; Dakhel and Mohammed 2011). One drug within this group, 5-FU, inhibits uracil metabolism, and has become increasingly popular since its development in the 1950s (Longley, Harkin, and Johnston 2003;Tanaka et al 2000).…”

Section: Introductionmentioning

confidence: 99%

Antioxidant and Anti-Inflammatory Effects of Myricetin on 5-Fluorouracil-Induced Hepatotoxicity in Male Rats

Hassan,

Al-Shawi

2024

Preprint

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5- Fluorouracil (5-FU) is widely-used as an anticancer drug to treat solid cancers, such as those of the colon, breast, rectum, and pancreas. However, its clinical application is limited due to its gastrointestinal and hematological toxicity. Myricetin (3, 3′, 4′, 5, 5′,7-hexahydroxyflavone) is a naturally-occurring flavanol found in fruits, vegetables, teas, and medicinal plants that has antimicrobial, antiviral, anti-aging, and anti-diabetic activities. The goal of this study was to evaluate the effect of two doses of myricetin on 5-flurouracil-induced hepatotoxicity in Wistar rats. Forty-two male Wistar rats were divided into six groups of seven rats each: Control (group 1) rats received distilled water daily for 20 days; group 2 rats were intraperitoneally (IP)-injected with a single toxic dose (150 mg/kg) of 5-FU on day 20; groups 3 and 4 rats orally-received either 25 or 50 mg/kg/day of myricetin, respectively, for 20 days. Group 5 and 6 rats orally-received 25 or 50 mg/kg/day of myricetin, respectively, for 20 days, and were IP-injected with 5-FU on day 20. From the results obtained from this study, it can be concluded that myricetin increases antioxidant levels and reduces liver inflammation, decreasing negative side-effects. The inclusion of myricetin with 5-FU resulted in positive histological changes that enhanced liver function.

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Section: Introductionmentioning

confidence: 99%

Antioxidant and Anti-Inflammatory Effects of Myricetin on 5-Fluorouracil-Induced Hepatotoxicity in Male Rats

Hassan,

Al-Shawi

2024

Preprint

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Synthesis, Characterization and Preliminary Anticancer Study of Novel 5-fluorouracil Conjugate with Pyrrolidine Dithiocarbamate as a Mutual Anticancer Prodrug

Shihab

Mohammed²

2019

IJPS

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5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds. ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed enhanced cytotoxic effects for [IV] over 5-FU.

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Synthesis and Characterizations of Dipeptide Derivative of Gentamicin

Khudair

Fatih²

2019

IJPS

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Abstract The target derivative are gentamicin linked with L-Val- L-Ala by an ester linkage. These were synthesized by esterification method, which included the reaction of -OH hydroxyl group on (carbon No.5) of gentamicin with the acid chloride of the corresponding dipeptide, The preparation of new derivative of gentamicin involved protected the primary & secondary amine groups of Gentamicin, by Ethylchloroformate (ECF) to give N-carbomethoxy Gentamicin which was used for further chemical synthesis involving the free hydroxyl groups. Then prepared dipeptide (L-Val- L-Ala) by conventional solution method in present DCC & HoBt then reacted with thionyl chloride to prepared acid chloride of dipeptides, then after, linked by ester linkage to N-protection gentamicin in present pyridine as base, finally deportation the amino group of synthesized compound by using TFAA in present anisole. The characterization of the titled compounds were performed utilizing FTIR spectroscopy, CHNS elemental analysis, and by measurements of their physical properties.

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Synthesis of 5-Fluorouracil Derivatives as Possible Mutual Prodrugs with Meloxicam and Ibuprofen for Targeting Cancer Tissues

Cited by 3 publications

References 15 publications

Antioxidant and Anti-Inflammatory Effects of Myricetin on 5-Fluorouracil-Induced Hepatotoxicity in Male Rats

Antioxidant and Anti-Inflammatory Effects of Myricetin on 5-Fluorouracil-Induced Hepatotoxicity in Male Rats

Synthesis, Characterization and Preliminary Anticancer Study of Novel 5-fluorouracil Conjugate with Pyrrolidine Dithiocarbamate as a Mutual Anticancer Prodrug

Synthesis and Characterizations of Dipeptide Derivative of Gentamicin

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