An investigative study of antitumor properties of a novel thiazolo[4,5-d]pyrimidine small molecule revealing superior antitumor activity with CDK1 selectivity and potent pro-apoptotic properties

Mohamed, Sameh H.; Elgiushy, Hossam R.; Taha, Heba; Hammad, Sherif F.; Aboutaleb, Nageh; Abouzid, Khaled A. M.; Al-Sawaf, H. A.; Hassan, Zeinab

doi:10.1016/j.bmc.2020.115633

Cited by 5 publications

(1 citation statement)

References 34 publications

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“…These structures, which especially help to understand life processes, have contributed to society in biological and industrial terms [2]. Some pyrimidine and fused heterocyclic pyrimidine derivatives have been reported to have a wide range of pharmacological properties, including activities such as antiviral [3], antitumor [4], antibacterial [5], antihypertensive [6], antioxidant [7], anticancer [8], and anti‐inflammatory [9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of new thiazine and thiazole derivatives via cyclization reactions; investigating their electronic properties and determination of antioxidant properties

Ergan

Tozlu

2022

Journal of Heterocyclic Chem

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4-[2,4-dimethoxyphenyl]-6-phenyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) (phenyl) methanone (1) have been prepared by Biginelli three-component cyclocondensation reaction of catalyzed with p-toluene sulfonic acid in ethanol. Pyrimido[2,1-b]thiazine (2) and thiazolo[3,2-a]pyrimidine (3) derivatives were obtained by a simple one-pot condensation reaction of starting compound 1 and 3-bromopropionic acid, bromoacetic acid and, respectively. By performing the reactions of compound 3 with heteroaromatic and aromatic aldehydes, arylidine-bicyclic thiazolo pyrimidine compounds (4-9) were synthesized. Theoretical calculations and molecular electrostatic potential maps of all synthesized compounds were performed using the Gaussian software package Density Functional Theory (DFT/6-31G: B3LYP). In addition, studies were carried out to determine the antioxidant properties of all the compounds obtained by the DPPH method, and compound 1 was found to be the most effective compound. The structures of the newly synthesized compounds were analyzed using spectroscopic methods such as IR, 1 H, and 13 C.

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