Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment

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Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment Publisher Pubmed

Shirvani P¹ ; Fayyazi N^{1, 2} ; Van Belle S³ ; Debyser Z³ ; Christ F³ ; Saghaie L¹ ; Fassihi A¹

Source: Bioorganic and Medicinal Chemistry Letters Published:2022

Abstract

Keeping in view the pharmacological properties of indolinones as promising scaffold as kinase inhibitors, herein, a novel series of 3-hydrazonoindolin-2-one derivatives bearing 3-hydroxy-4-pyridinone moiety were synthesized, studied by molecular docking, and fully characterized by spectroscopic techniques. All the prepared compounds were evaluated for their cytotoxicity attributes against a panel of tumor cell lines, including non-small cell lung cancer (A549), breast carcinoma (MCF-7), acute myeloid leukemia (AML), and chronic myeloid leukemia (CML). They displayed moderate to promising antiproliferative effects toward A549 and MCF-7 cells but remarkable results against AML and CML. Especially, compound 10k was found to be more potent against AML (EC50 = 0.69 μM) compare to the other halogen-substituted derivatives. FMS-like tyrosine kinase 3 (FLT3) is known to be expressed in AML cancer cells. The molecular docking studies demonstrated that our prepared compounds were potentially bound to AML active site through essential H-bond and other vital interactions with critical binding residues. © 2022

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Style	Citing Format
MLA	Shirvani P, et al.. "Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment." Bioorganic and Medicinal Chemistry Letters, vol. 70, no. , 2022, pp. -.
APA	Shirvani P, Fayyazi N, Van Belle S, Debyser Z, Christ F, Saghaie L, Fassihi A (2022). Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment. Bioorganic and Medicinal Chemistry Letters, 70(), -.
Chicago	Shirvani P, Fayyazi N, Van Belle S, Debyser Z, Christ F, Saghaie L, Fassihi A. "Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment." Bioorganic and Medicinal Chemistry Letters 70, no. (2022): -.
Harvard	Shirvani P et al. (2022) 'Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment', Bioorganic and Medicinal Chemistry Letters, 70(), pp. -.
Vancouver	Shirvani P, Fayyazi N, Van Belle S, Debyser Z, Christ F, Saghaie L, et al.. Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment. Bioorganic and Medicinal Chemistry Letters. 2022;70():-.
BibTex	@article{ author = {Shirvani P and Fayyazi N and Van Belle S and Debyser Z and Christ F and Saghaie L and Fassihi A}, title = {Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment}, journal = {Bioorganic and Medicinal Chemistry Letters}, volume = {70}, number = {}, pages = {-}, year = {2022} }
RIS	TY - JOUR AU - Shirvani P AU - Fayyazi N AU - Van Belle S AU - Debyser Z AU - Christ F AU - Saghaie L AU - Fassihi A TI - Design, Synthesis, in Silico Studies, and Antiproliferative Evaluations of Novel Indolin-2-One Derivatives Containing 3-Hydroxy-4-Pyridinone Fragment JO - Bioorganic and Medicinal Chemistry Letters VL - 70 IS - SP - EP - PY - 2022 ER -

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