Discovery of new pyrimido[5,4-c]quinolines as potential antiproliferative agents with multitarget actions: Rapid synthesis, docking, and ADME studies

• Published in: Bioorganic chemistry Vol. 121; p. 105693
• Main Authors: Mekheimer, Ramadan A., Allam, Samar M.R., Al-Sheikh, Mariam A., Moustafa, Moustafa S., Al-Mousawi, Saleh M., Mostafa, Yaser A., Youssif, Bahaa G.M., Gomaa, Hesham A.M., Hayallah, Alaa M., Abdelaziz, Mohamed, Sadek, Kamal U.
• Format: Journal Article
• Language: English
• Published: SAN DIEGO Elsevier Inc 01.04.2022; Elsevier
• Subjects: Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Biochemistry & Molecular Biology; CDK2; Cell Line, Tumor; Cell Proliferation; Chemistry; Chemistry, Organic; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; EGFR; ErbB Receptors; Life Sciences & Biomedicine; Molecular Docking Simulation; Molecular Structure; Physical Sciences; Pyrimidine; Quinoline; Quinolines - pharmacology; Science & Technology; Structure-Activity Relationship; Synthesis; Topo; Quinoline; Synthesis; Topo; EGFR; CDK2; Pyrimidine; DRUG DISCOVERY; TOPOISOMERASE-I; CYCLIN-DEPENDENT KINASE; RING-SYSTEMS; ANTITUMOR; SOLUBILITY; INHIBITION; BIOLOGICAL EVALUATION; FUSED QUINOLINE-HETEROCYCLES; DERIVATIVES

[Display omitted] A novel series of pyrimido[5,4-c]quinoline derivatives variously substituted at positions 2 and 5 have been synthesized, in good to excellent yields, via rapid base-catalyzed cyclization reaction of 2,4-dichloroquinoline-3-carbonitrile (5) with guanidine hydrochlorides 6a-c. All th...