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Paper | Regular issue | Vol 102, No. 5, 2021, pp.930-940
Published online, 3rd March, 2021
DOI: 10.3987/COM-21-14426
One-Pot and Three-Component Synthesis of Some Novel Functionalized Chromonyl Pyrido[2,3-d]pyrimidines as Anticancer Agents

Tarik E. Ali,* Mohammed A. Assiri, Ali A. Shati, Mohammad Y. Alfaifi, Serag Eldin I. Elbehairi, and Attalla F. El-Kott

*Department of Chemistry, Faculty of Education, Ain Shams University, Roxy, Cairo, Egypt


A facile and efficient method for the construction of functionalized chromonyl pyrido[2,3-d]pyrimidines via a one-pot, three-component reaction of 6-aminothiouracil and 4,6-diaminopyrimidine-2(1H)-thione with 4-oxo-4H-chromene-3-carboxaldehyde in the presence of different nitrile active methylene compounds in distillated water at 70 oC without using a catalyst was achieved. The methodology displayed excellent yields and simple workup procedure. The targeted compounds were assessed for their in vitro anticancer activity against mammary gland breast cancer cell line (MCF-7), liver cancer (HepG-2), and human colon cancer (HCT-116) by using sulphorhodamine B assay (SRB) method, while doxorubicin, was utilized as standard reference drug. Compounds 4b and 6a were the best potent cytotoxic agents towards liver (HepG-2) and colon (HCT-116) compared with doxorubicin as a reference drug with IC50 values ranging from 1.1 to 1.8 μg/mL.