SYNTHESIS OF SOME PYRIMIDO-[1,6-a]- INDOLE OF POTENTIAL PHARMACOLOGICAL INTEREST

Ebeid, Mohamed; Lashine, Sayed; El-Adl, Sobhy M.; Abou-Kull, Mansour

doi:10.21608/zjps.1994.186442

Cited by 5 publications

(1 citation statement)

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“…It was reported that the indole structure has emerged as one of the most important synthetic sources for therapeutic drugs 4 – 6 . It has been reported that indole-containing compounds possess a wide range of bioactivities such as antimicrobial 7 , anticancer 8 – 10 antihypertensive 11 antimalarial 12 , analgesic 13 , antidiabetic 14 , anti-inflammatory 15 – 17 , and anti-HIV activities 18 . Fan Zhang et al, reported the promising anti-tumour activity of 2-amino-3-cyano-6-(1 H -indol-3-yl)-4-phenylpyridine derivatives against four human cancer cell lines (H460, A549, HT-29 and SMMC-7721) 19 .…”

Section: Introductionmentioning

confidence: 99%

Novel 3-(pyrazol-4-yl)-2-(1H-indole-3-carbonyl)acrylonitrile derivatives induce intrinsic and extrinsic apoptotic death mediated P53 in HCT116 colon carcinoma

Mohamed,

Ibrahim,

Saddiq

et al. 2023

Sci Rep

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A novel series of α-cyano indolylchalcones was prepared, and their chemical structures were confirmed based on the different spectral data. Among them, compound 7f was observed to be the most effective bioactive chalcone with distinguished potency and selectivity against colorectal carcinoma (HCT116) with IC50 value (6.76 µg/mL) relative to the positive control (5 FU) (77.15 µg/mL). In a preliminary action study, the acrylonitrile chalcone 7f was found to enhance apoptotic action via different mechanisms like inhibition of some anti-apoptotic protein expression, regulation of some apoptotic proteins, production of caspases, and cell cycle arrest. All mechanisms suggested that compound 7f could act as a professional chemotherapeutic agent. Also, a molecular docking study was achieved on some selected proteins implicated in cancer (Caspase 9, XIAP, P53 mutant Y220C, and MDM2) which showed variable interactions with compound 7f with good Gibbs free energy scores.

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Section: Introductionmentioning

confidence: 99%

Novel 3-(pyrazol-4-yl)-2-(1H-indole-3-carbonyl)acrylonitrile derivatives induce intrinsic and extrinsic apoptotic death mediated P53 in HCT116 colon carcinoma

Mohamed,

Ibrahim,

Saddiq

et al. 2023

Sci Rep

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Synthesis of Some New Fused Pyrazole Derivatives Bearing Indole Moiety as Antioxidant Agents

El‐Mekabaty

Etman

Mosbah

2015

Journal of Heterocyclic Chem

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3‐(1H‐Indol‐3‐yl)‐1H‐pyrazol‐5‐amine 3 was prepared in a quantitative yield by heating 3‐(1H‐indol‐3‐yl)‐3‐oxopropanenitrile 2 in dry ethanol with hydrazine hydrate, and utilized as key intermediate for the synthesis of some new pyrazolo[1,5‐a]pyrimidines and pyrazolo[5,1‐c]triazines. Structures of the newly synthesized compounds were established by elemental analysis and spectral data and evaluated as antioxidant agents. Most of the tested compounds belonging to the pyrazolo[1,5‐a]pyrimidine series exhibited better activities than members of the pyrazolotriazine one.

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A multicomponent reaction to design antimalarial pyridyl-indole derivatives: Synthesis, biological activities and molecular docking

Elshemy

Zaki

Mohamed

et al. 2020

Bioorganic Chemistry

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SYNTHESIS OF SOME PYRIMIDO-[1,6-a]- INDOLE OF POTENTIAL PHARMACOLOGICAL INTEREST

Cited by 5 publications

References 0 publications

Novel 3-(pyrazol-4-yl)-2-(1H-indole-3-carbonyl)acrylonitrile derivatives induce intrinsic and extrinsic apoptotic death mediated P53 in HCT116 colon carcinoma

Novel 3-(pyrazol-4-yl)-2-(1H-indole-3-carbonyl)acrylonitrile derivatives induce intrinsic and extrinsic apoptotic death mediated P53 in HCT116 colon carcinoma

Synthesis of Some New Fused Pyrazole Derivatives Bearing Indole Moiety as Antioxidant Agents

A multicomponent reaction to design antimalarial pyridyl-indole derivatives: Synthesis, biological activities and molecular docking

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