Green and Efficient Synthesis of Some Pyrido[2,3-D]Pyrimidin-4(3h)-One Derivatives Via Iodine Catalyst in Aqueous Media and Evaluation the Synthesized Compounds as Anticancer

Abstract

(2), 3-amino derivative 3a, 3b and hydroxy derivative 3c displayed the highest activity among the test compounds with IC50 < 5 mg/mL

Synthesis and Anticancer Perspective of Pyridopyrimidine Scaffold - An Overview

“…Hala B et al, [16] stated pyrido [2,3-d] pyrimidines and fused [1,2,4]triazolo[4,3-a]pyrimidine derivatives, which were reported for anti-tumour activity [14][15][16][17][18][19][20][21][22][23][24][25]. These two groups upon combination results in the formation of tricyclic ring system containing pyridine, triazole and pyrimidines (i.e pyrido [2,3-d [1,2,4] triazolo [4,3-a] pyrimidine) and the resulting impact on the biological activities are delighted [26][27][28][29][30][31][32].…”

“…The starting compounds (1-4) undergo the direct condensation with urea at 260-300 0 C result in the formation of the target compound i.e "4amino-5,7-disubstituted-pyrido [2,3-d]pyrimidine-2(1H)-ones" (24)(25)(26)(27).…”

“…Nicotinonitriles (1)(2)(3)(4)(5), were cyclized by using different reagents results in the formation of bicyclic "pyrido [2,3-d]pyrimidines" (6-10), (11)(12)(13)(14)(15), (16)(17)(18)(19)(20), and (24-27) with different substitution, where most of them were inactive against all 3 tested cell lines, Further, ketone group present at 2nd position is isostatically replaced with thione group in pyrido [2,3d]pyrimidine-2(1H)-ones (24)(25)(26)(27), resulted in two weakly active molecules, namely, 30 (X = Br; R = 3,4-(OCH 2 O)C 6 H 3 ) and 32 (X = OCH 3 ; R=2thienyl). But further improved cytotoxic activity was observed by the thioalkylation of that 2thione group of (28-32) mainly with methyl or ethyl group yields potentially active molecules 33, 34, 36, and 37.…”

“…Based on the literature, Ayman M. F. Elgohary et al [25] reported pyrido [2,3-d]pyrimidine nucleus present in a variety of active compounds since it exhibits different biological properties including antitumor activity [8,14,23,56,57]. They have synthesized new "2propylpyrido[2,3-d]pyrimidin-4(3H)-one" derivatives possessing various substituents at 3 rd position, like NH 2 and N-aryl groups mainly to examine the effect of particular substituents on antitumor activity.…”

Design, Synthesis And Evaluation Of New Chemosensors Containing Quinazolinones Moiety For Ions In An Aqueous Medium And Biological Samples

“…Hence, the significance of producing chemosensors carrying quinazolinone moiety is increasing the selective and specific activity of the sensor. As an extension of our awareness in the Synthesis of heterocyclic compounds, namely pyridopyrimidine 44 and quinazolinone 45 , here we synthesize quinazolinone derivatives that have selectivity to react with ions in aqueous and biological samples.…”