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Background: Since CDKs have been demonstrated to be overexpressed in a wide spectrum of human malignancies, their inhibition has been cited as an effective technique for anticancer drug development.

Methods: In this context, new bis-oxindole/spiro-triazole-oxindole anti-breast cancer drugs with potential CDK4 inhibitory effects were produced in this work. The novel series of bis-oxindole/spirotriazole- oxindole were synthesized from the reaction of bis-oxindole with the aniline derivatives then followed by 1,3-dipolar cycloaddition of hydrazonoyl chloride.

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Group VA metalloid ion Lewis acids, Sb(v) was identified as a highly potent catalyst for the one-pot three-component synthesis of bis-spiro piperidine derivatives. The reaction was performed using amines, formaldehyde, and dimedone under ultrasonic irradiation at room temperature. The strong acidic property of the nano γ-alumina supported antimony(v) chloride plays a key role in accelerating the rate of the reaction and initiates the reaction smoothly.

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Synthesis of bis-spiro-oxetane and bis-spiro-tetrahydrofuran pyrroline nitroxide radicals relies on the Mitsunobu reaction-mediated double cyclizations of -Boc protected pyrroline tetraols. Structures of the nitroxide radicals are supported by X-ray crystallography. In a trehalose/sucrose matrix at room temperature, the bis-spiro-oxetane nitroxide radical possesses electron spin coherence time, ≈ 0.

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A diastereoselective formal 1,6-conjugate-addition-mediated [2 + 1] annulation reaction using -quinone methides and pyrazolones has been described. The corresponding bis-spiro[cyclohexadienone-cyclopropane-pyrazolone] compounds were obtained in very good yield under mild reaction conditions.

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First Synthesis for Bis-Spirothiazolidine Derivatives as a Novel Heterocyclic Framework and Their Biological Activity.

Mini Rev Med Chem

October 2020

Department of Photochemistry, Chemical Industries Research Division, National Research Centre, 33 EL-Bohouth St., Dokki 12622, Giza, Egypt.

Background: Spirothiazolidines are versatile synthetic scaffold possessing wide spectrum of biological interests involving potential anticancer activity.

Objective: To report the first synthesis of Bis Spiro-thiazolidine as a novel heterocyclic ring system.

Methods: One-pot three-component reaction including condensation of p-phenyllene diamine; cyclohexanone and thioglycolic acid produced Spiro-thiazolidine 4, which underwent further condensation with cyclohexanone and thioglycolic acid with equimolar ratio to introduce Bis-Spiothiazolidine 5 as the first synthesis.

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