Synthesis of Novel Heterocyclic Compounds for Antitumor and Radioprotective Activities

Ghorab, Mostafa M.; Hassan, Aisha Y.; Nassar, O.M.

doi:10.1080/10426509808545486

Cited by 15 publications

(5 citation statements)

References 13 publications

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“…Interaction of 3-amino-4-methyl-6-phenyl thieno [2,3-b] pyridine-2carboxamide 10 [13], with triethyl orthoforamate or formic acid [5,6] gave pyrido thieno pyrimidinone derivative 11. The chloro compound 12 was synthesized by refluxing the pyrimidinone 11 in phosphorous oxychloride.…”

Section: Resultsmentioning

confidence: 99%

SYNTHESIS AND REACTIONS OF SOME PYRIDINE AND THIENO [2,3-b] PYRIDINE DERIVATIVES WITH EXPECTED BIOLOGICAL ACTIVITY

Hassan

Fayz²

2008

Al-Azhar Bulletin of Science

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A synthesis of pyridine-2(1H)-thione derivative 2 and thieno-[2,3-b] -pyridine derivatives 4,5 utilizing cyanothioacetamide and arylhydrazone of benzoylacetone 1 as starting compounds is described. Pyridinethione derivative 6 reacted with aromatic aldehyde to give styrylpyridinethione derivative 7. Compound 7 was reacted with chloroacetone to obtain thienopyridine derivative 8. Cycloaddition reaction was carried out on 8 with dienophiles, to afford the corresponding cycloadduct 9. Pyridinethione derivative 6 reacted with halogen-containing materials to give the corresponding thienopyridine derivatives 10, 17. the reaction of 10 with triethyl orthoformate or formic acid led to the formation of pyridothienopyrimdine derivative 11. The hydrazino derivative 13, gave with triethyl orthoformate triazolo-pyrimidothienopyridine derivative 14. Compound 10 reacted with nitrous acid to gave pyridothienotrizinone derivative 15. Thienopyridine derivative 17 reacted with triethyl orthoformate to give 18. Triazipinopyrimidothienopyridine derivative 20 obtained from compound 18 after reaction with hydrazine hydrate and acetylacetone. Compound 17 reacted with carbon disulfide to give pyrimidinedithione derivative 21.

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Section: Resultsmentioning

confidence: 99%

SYNTHESIS AND REACTIONS OF SOME PYRIDINE AND THIENO [2,3-b] PYRIDINE DERIVATIVES WITH EXPECTED BIOLOGICAL ACTIVITY

Hassan

Fayz²

2008

Al-Azhar Bulletin of Science

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“…2-(7,9-Dimethylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4-yl)-5-methyl-2,4-dihydro-3H-pyrazol-3-one (13). A mixture of ethylacetoacetate (0.78 g, 6 mmol) and (1) (0.98 g, 4 mmol) was refluxed in absolute ethanol (30 mL) for 9 h. The resulting precipitate was filtered off with suction, washed with ethanol, and recrystallized from ethanol to give a powder of (13) (84%), mp 237−239 °C.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

“…In addition to antimicrobial, − anticonvulsant, and anticancer activities − of pyridothienopyrimidine derivatives, recent studies showed that they have the ability to specifically activate testicular steroidogenesis without affecting thyroid functions . They also have inhibitory effects on some closely linked factors to human malignancies such as cellular mesenchymal–epithelial transition factor; the Moloney murine leukemia virus-1 (pim-1) proviral integration site; some signaling pathways that play an important role in tumorigenesis; VEGFR-2 receptors to reduce angiogenesis or lymphangiogenesis; and act as alpha-1 blockers that are mainly used as a prescribed drugs for benign prostatic hyperplasia, manage hypertension, and treatment of posttraumatic stress disorder.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antibacterial Activities of Different Five-Membered Heterocyclic Rings Incorporated with Pyridothienopyrimidine

2020

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d]pyrimidine (1) is a reported pyridothienopyrimidine derivative. In the current study, (1) has been reacted with different reagents to obtain 12 new pyridothienopyrimidine derivatives. The newly synthesized five-membered heterocyclic rings incorporated with pyridothienopyrimidines have been screened for their antibacterial activities. The results encourage further studies on other possible biological activities.

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“…Later, in vivo anorectic action activity of isothiazolo [5, 4-b]pyridine derivatives was reported by Malinka and Rutkowska [263]. There have been a few reports on bioactivity of isothiazolopyridine derivatives such as antitumor and radioprotective activities, in vitro antibacterial activity, analgesic activity, cyclin G-associated kinase inhibition, antiviral activity, and COX-1/2 inhibitory activity [264][265][266][267][268][269].…”

Section: Thiazolopyridines and Isothiazolopyridinesmentioning

confidence: 99%

Fused Pyridine Derivatives: Synthesis and Biological Activities

Istanbullu¹,

Bayraktar²,

Saylam³

2023

Exploring Chemistry With Pyridine Derivatives

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Five-membered heteroaromatic ring fused pyridine derivatives are of increasing interest in drug design and medicinal chemistry. The structural similarity of many drugs (especially antiviral and anticancer ones) with DNA bases such as adenine and guanine is a key factor to explain their effectiveness. Apart from these, it is also found in the structures of substances with antituberculosis, antibacterial, antifungal, anti-inflammatory, and antimalarial activities. Another advantage of this group of compounds is their positive contribution to solubility, polarity, lipophilicity, and hydrogen bonding capacity properties of the compounds they are incorporated into. In this chapter, various bioactivities of fused pyridine derivatives will be categorized and summarized.

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Synthesis of Novel Heterocyclic Compounds for Antitumor and Radioprotective Activities

Cited by 15 publications

References 13 publications

SYNTHESIS AND REACTIONS OF SOME PYRIDINE AND THIENO [2,3-b] PYRIDINE DERIVATIVES WITH EXPECTED BIOLOGICAL ACTIVITY

SYNTHESIS AND REACTIONS OF SOME PYRIDINE AND THIENO [2,3-b] PYRIDINE DERIVATIVES WITH EXPECTED BIOLOGICAL ACTIVITY

Synthesis and Antibacterial Activities of Different Five-Membered Heterocyclic Rings Incorporated with Pyridothienopyrimidine

Fused Pyridine Derivatives: Synthesis and Biological Activities

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